The 31st Medicinal Chemistry Symposium Scientific Program Poster Presentation Day1 (1P-01～67) 1P-01 Synthesis and Biological Activity of 3',5'-Difluorothalidomides

Mayaka Maeno1*, Hiromi Taira2, Etsuko Tokunaga2, Norio Shibata1,2 (1Department of Nanopharmaceutical Science, Graduate School of Engineering, Nagoya Institute of Technology, 2Department of Frontier Materials, Graduate School of Engineering, Nagoya Institute of Technology)

1P-02 Stereoselective synthesis and biological activity of 19-norvitamin D derivatives having conjugated diyne and adamantyl group on the side chain Yusuke Watarai1*, Kazuki Maekawa1, Michiyasu Ishizawa2, Shigeyuki Uno2, Mourino Antonio3, Makoto Makishima2, Hiroaki Tokiwa1, Sachiko Yamada2 (1college of science, Rikkyo University, 2school of medicine, Nihon University, 3department of chemistry, University of Santiago de Compostela)

1P-03 2‐Pyridone Synthesis Using 2‐(Phenylsulfinyl)acetamide Masaya Fujii1,2*, Takuya Nishimura1, Takahiro Koshiba1, Satoshi Yokoshima2, Tohru Fukuyama2 (1Graduate School of Pharmaceutical Sciences, the University of Tokyo, 2Graduate School of Pharmaceutical Sciences, Nagoya University)

1P-04 Regioselective trifluoromethylation of N-heteroaromatic compounds using BF2CF3 activator Tomoaki Nishida1*, Haruka Ida1, Yoichiro Kuninobu1,2, Motomu Kanai1,2 (1Graduate School of Pharmaceutical Sciences, The University of Tokyo, 2ERATO-JST)

1P-05 Development of the efficient synthetic method of benzofuro[2,3-b]pyrroles Masafumi Ueda, Yuta Ito, Tetsuya Miyoshi, Okiko Miyata (Kobe Pharmaceutical University)

1P-06 Process Resaerch Development on the New C-Piperazinyl Drug Drug Substances (3) Yasuhiro Torisawa1*, Minoru Yasuda2, Yasuhiro Takahasi2 etc (1Takasaki University of H&W, 2DNP Fine Chemical Utsunomiya)

1P-07 Innovative Analytical Techniques for Reaction Monitoring and Process Optimization Masayo Yabu1*, Shinnosuke Horie1, Michael D. Jones2, Sean M. McCarthy2 (1Nihon Waters K.K., 2Waters Corporation)

1P-08 Design and synthesis of Arg derivatives for stabilized helical cell-penetrating peptides Yosuke Demizu1*, Norikazu Yamazaki1, Hiroko Yamashita1,2, Yukiko Sato1, Makoto Oba3, Masakazu Tanaka3, Masaaki Kurihara1,2 (1National Institute of Health Sciences, 2Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, 3Graduate School of Biomedical Sciences, Nagasaki University)

1P-09 Development of Myostatin Inhibitory Peptides for Enhancement of Muscle Function 1: Structure-Activity Relationship Study Using Alanine Scanning Shota Takayama1*, Kentaro Takayama1, Yuri Noguchi2, Shin Aoki1, Tomo Asari1,

Yusaku Mino1, Akihiro Taguchi1, Fumika Yakushiji1, Yutaka Ohsawa3, Yoshihide Sunada3, Fumiko Itoh2, Yoshio Hayashi1 (1Department of Medicinal Chemistry and 2Laboratory of Cardiovascular Medicine, Tokyo University of Pharmacy and Life Sciences, 3Department of Neurology, Kawasaki Medical School)

1P-10 Synthesis and Biological Evaluation of Destruxin E and its Derivatives as Negative Regulators of Osteoclast Morphology Hiroshi Sato1,2*, Yoshitaka Ishida1, Masahito Yoshida1, Hayato, Murase3, Hiroshi Nakagawa3, Takayuki Doi1 (1Graduate School of Pharmaceutical Sciences, Tohoku University, 2Mitsubishi Tanabe Pharma Corporation, 3Department of Applied Biological Chemistry, Chubu University)

1P-11 Structure activity relationship of citridone A Kenta Shimoyama*, Takashi Fukuda, Hiroshi Tomoda, Tohru Nagamitsu (Granduate School of Pharmaceutical Science, Kitasato University)

1P-12 Structure-activity relationship studies of nafuredin-γ Risa Shimizu*, Eri Shimizu, Masaki Ohtawa, Shiho Arima, Satoshi Omura, Tohru Nagamitsu（Graduate School of Pharmacy Sciences, Kitasato University）

1P-13 Design and synthesis of truncated analogs of pyripyropene A as potent ACAT2 inhibitors Masaki Ohtawa*, Tomiaki Terayama, Taichi Ohshiro, Takashi Fukuda, Satoshi Omura, Hiroshi Tomoda, Tohru Nagamitsu (Graduate School of Pharmaceutical Sciences, Kitasato University)

1P-14 Synthesis and ABCG2 Inhibitory Evaluation of 5-N-Acetylardeemin Dervertives Daigo Hayashi*, Naoki Tsukioka, Yoshiki Matsubayashi, Yutaka Inoue, Kazuhiro Higuchi, Yoji Ikegami, Tomomi Kawasaki (Meiji Pharmaceutical University)

1P-15 Structure-activity Relation study of Matrine-type Alkaloids Part21 : Synthesis and Antinociception of 3-Phenylpiperidine derivatives. Hiroyoshi Teramoto*, Junichi Koizumi, Toshiyuki Shimekake, Kenta Kawashima, Shigeru Sasaki, Takayasu Yamauchi, Kimio Higashiyama(Institute of Medicinal Chemistry, Hoshi University)

1P-16 Inhibitory constituents on melanogenesis from Sri Lankan curry-leaf, the leaves of Murraya koenigii Seikou Nakamura1*, Souichi Nakashima1,2, Yoshimi Oda1,2, Nami Yokota1, Takahiro Matsumoto1, Tomoe Ohta1, Keiko Ogawa1, Masayuki Yoshikawa1, Hisashi Matsuda1 (1Kyoto Pharmaceutical University, 2N.T.H Co., Ltd.)

1P-17 Reducing effects of seeds of Nigella sativa on triglyceride content in mouse liver Kiyofumi Ninomiya1*, Naomichi Okumura1, Osamu Muraoka1, Fengmin Xu2, Hisashi Matsuda2, Masayuki Yoshikawa2, Takao Hayakawa1, Toshio Morikawa1 (1Pharmaceutical Research and Technology Institute, Kinki University, 2Kyoto Pharmaceutical University)

1P-18 Structure-activity Rerationships of Thiophen Analoues of Annonaceous Acetogenins Naoto Kojima1*, Tetsuya Fushimi2, Takahiro Tatsukawa2, Tetsuaki Tanaka2, Mutsumi Okamura3, Shingo Dan3, Takao Yamori3, Hiroki Iwasaki1, Masayuki Yamashita1 (1Kyoto Pharmaceutical University, 2Graduate School of

Pharmaceutical Sciences, Osaka University, 3Cancer Chemotherapy Center, Japanese Foundation for Cancer Research)

1P-19 Methanesulfonyl Group as a Useful Substituent for Reduction of hERG Inhibition: QSAR Studies on a Series of Phenylazoleanilide Derivatives Hiroyuki Ushio1*, Mikiko Aoto2, Seigo Ishibuchi2, Naoto Fujie2, Masayuki Watanabe2, Maiko Hamada2, Noriyasu Seki3, Noriko Sato3, Kunio Sugahara3, Toshinobu Shimizu4, Kunitomo Adachi2* (1Process Chemistry Research Laboratories, CMC Division, 2Medicinal Chemistry Research Laboratories I, 3Pharmacology Research Laboratories I, 4Safety Research Laboratories, Research Division, Mitsubishi Tanabe Pharma Corporation)

1P-20 3D-QSAR analyses for κ/µ-selectivities of opioid agonists Noriyuki Yamaotsu1*, Hiroshi Nagase2, Hideaki Fujii1, Shuichi Hirono1 (1School of Pharmacy, Kitasato University, 2International Institute for Integrative Sleep Medicine, University of Tsukuba)

1P-21 Computational analysis of the difference in inhibitory activities of α-glucosidase inhibitors against human and rat enzymes Kazuko Shimada, Shinya Nakamura, Genzoh Tanabe, Osamu Muraoka, Isao Nakanishi（Faculty of Pharmacy, Kinki university）

1P-22 Theoretical Study of DPP-4 Inhibitors bassed on the First-Principles Calculations 2 Erika Ishitsubo1, Yuka Nakano2, Hiroaki Tokiwa1,2* (1Department of Chemistry, Rikkyo University, 2Research Center for Smart Molecules, Rikkyo University)

1P-23 Identification of SUMO activating enzyme 1 inhibitors utilizing virtual screening approach Ashutosh Kumar1, Akihiro Ito2, Mikako Hirohama2, Minoru Yoshida2 and Kam Y. J. Zhang1* (1Zhang Initiative Research Unit, Institute laboratories, RIKEN, 2Chemical Genetics Laboratory/Chemical Genomics Research Group, RIKEN)

1P-24 Development of a novel dimethylnitrobenzene-type nitric oxide donor controllable with visible yellow-green light irradiation Kai Kitamura1*, Kazuhiro Hishikawa1, Naoya Ieda1, Takayoshi Suzuki2, Naoki Miyata1, Hidehiko Nakagawa1,3 （1Graduate School of Pharmaceutical Sciences, Nagoya City University, 2Graduate School of Medical Science Kyoto Prefectural University of Medicine, 3PRESTO, Japan Science and Technology Agency）

1P-25 Nucleobase-polyamine conjugates for specific cleavage of the abasic site of DNA Yukiko Abe*, Rie Yamaguchi, Shigeki Sasaki (Graduate School of Pharmaceutical Sciences, Kyushu University)

1P-26 Basic evaluation of novel microwave reactor for synthesis of molecular imaging drugs Yusuke Yagi1, Hiroyuki Kimura1, Noriyuki Ooneda2, Hiromichi Odajima2, Masahiro Ono1, Hideo Saji1 (1Graduate School of Pharmaceutical Science, Kyoto University, 2Saida FDS Co., Ltd)

1P-27 Efficient Synthesis of Catechin Probe and its Molecular Toshiyuki Kan1*, Tomohiro Asakawa1, Kosuke Shimizu1, Naoto Oku1, Norihiro Harada2, Hideo Tsukada2 (1School of Pharmaceutical Sciences, University of Shizuoka, 2Central Research Laboratory, Hamamatsu Photonics K. K.)

1P-28 Development of radio-labeled probes targeting prostate-specific membrane antigen: structure-activity relationship and in vivo biodistribution studies Naoya Harada*, Hiroyuki Kimura, Satoru Onoe, Masahiro Ono, Hideo Saji (Graduate School of Pharmaceutical Sciences, Kyoto University)

1P-29 Study on radiopharmaceutical synthesis for the brain disease early detection Hiroshi Yamaguchi* (Radiology, Akita Research Institute for Brain and Blood Vessels)

1P-30 PPARγ agonistic effect of hesperidin metabolites Kanae Gamo1,2*, Minoru Waki1, Kenji Matsuno1, Hiroyuki Miyachi1, Nobuyasu Matsuura2 (1Department of Life Science, Faculty of Science, Okayama University of Science, 2Department of pharmaceutical Science, Graduate School of Medicine, Density and pharmaceutical Science, Okayama University)

1P-31 Peroxisome proliferator-activated receptor delta antagonists inhibit hepatitis C virus RNA replication Shintaro Ban*, Youki Ueda, Masao Ohashi, Kenji Matsuno, Masanori Ikeda, Nobuyuki Kato, Hiroyuki Miyachi (Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University)

1P-32 Development of novel progesterone receptor antagonists bearing a spherical hydrophobic structure Shuichi Mori1*, Yuki Takeuchi1, Eiichi Nakano1, Shinya Fujii1, Aya Tanatani2, Hiroyuki Kagechika1 (1Institute of Biomaterial and Bioengineering, Tokyo Medical and Dental University, 2Department of Chemistry Faculty of Science, Ochanomizu University)

1P-33 Relationships between Position of the Carbon Atoms on the Carborane Cage and Anti-androgen Activity in Carboranyl Phenyl Glycerol Derivatives Asako Kaise*, Takatoshi Abe, Kiminori Ohta, Yasuyuki Endo (Tohoku Pharmaceutical University)

1P-34 Development of novel selective estrogen receptor down-regulator (SERD) that possess endoxifen scaffold Masashi Kato1,2, Takuji Shoda1, Keiichiro Okuhira1, Hideshi Inoue2, Mikihiko Naito1, Masaaki Kurihara1,3 (1National Institute of Health Sciences, 2Graduate School of Life Science, Tokyo University of Pharmacy and Life Science, 3Graduate school of Bioscience and Biotechnology, Tokyo Institute of Technology)

1P-35 Discovery of Novel Series P2X3 Receptor Antagonists: Synthesis and Structure-Activity Relationships of Pyrrolinone Derivatives Hiroyuki Tobinaga*, Kentarou Asahi, Takayuki Kameyama, Tohru Horiguchi, Miho Oohara, Yukio Tada, Naoko Kurihara, Yasuhiko Kanda, Maki Tomari, Yoshikazu Tanaka, Fumiyo Takahashi, Shigenori Yagi, Emiko Shigetoshi, Yukio Takahara, Shinji Shimada, Chie Takeyama, Hiroki Tsuji, Shoichi Yamamoto, Shunji Shinohara, and Hiroyuki Kai (Shionogi & Co., Ltd.)

1P-36 Novel Xanthine Oxidase Inhibitors with triazine skeleton Kiminori Ohta, Yasuhiro Ishii, Yasuyuki Endo (Tohoku Pharmaceutical University)

1P-37 Discovery of Novel ALK5 Selective Inhibitors with a 4-Thiazolylimidazole Scaffold Hideaki Amada*, Yoshinori Sekiguchi, Naoya Ono, Takeshi Koami, Tetsuo Takayama,Tetsuya Yabuuchi, Hironori Katakai, Akiko Ikeda, Mari Aoki,

Takumi Naruse, Reiko Wada, Akiko Nozoe, Masakazu Sato (Taisho Pharmaceutical Co., Ltd.)

1P-38 Discovery of DF-461, a Potent Squalene Synthase Inhibitor Masanori Ichikawa*, Masami Ohtsuka, Hitoshi Ohki, Masahiro Ota, Noriyasu Haginoya, Masao Itoh, Yoshihiro Shibata, Kazuyuki Sugita, Yutaka Ishigai, Koji Terayama, Akira Kanda and Hiroyuki Usui

1P-39 Synthesis and structure activity relationships of hexafluoroisopropylbenzamide analogues as anti-hepatitis C virus agent Kenji MATSUNO,* Youki UEDA, Kenji ONODA, Miwa FUKUDA, Masanori IKEDA, Nobuyuki KATO, and Hiroyuki MIYACHI (Graduate School of Medicine, Dentistry and Pharmaceutical Sciences)

1P-40 Synthetic Studies on Anti-HCV Agents via Chemical Transformation of Cyclosporin Analogues (1) Takuya Makino*, Toshio Yamanaka, Seiji Yoshimura, Masae Sawada, Eisaku Tsujii, Masaichi Warizaya, Masahiro Neya, David Barrett (Astellas Phama Inc. )

1P-41 Synthetic Studies on anti-HCV Agents via Chemical Transformation of Cyclosporin Analogues (2) Toshio Yamanaka1*, Junya Ishida1, Ayako Toda1, Yu Harayama1, Takuya Makino1, Shigeki Kunikawa1, Masae Sawada1, Daisuke Tanabe1, Shinya Okuda2, Ohki Hidenori1, David Barrett1 (1Astellas Pharma Inc., 2Astellas Research Technologies Co., Ltd.)

1P-42 Synthesis and evaluation of phosphatidylinositol phosphate derivatives aiming at inhibition of HIV-1 release Hiroshi Tateishi1*, Kensaku Anraku2, Ryoko Koga3, Yoshinari Okamoto3, Mikako Fujita4, Masami Otsuka1（1Graduate School of Pharmaceutical Sciences, Kumamoto University, 2Institute of Health Sciences, Kumamoto Health Science University, 3Faculty of Life Sciences, School of Pharmacy, Kumamoto University, 4Research Institute for drug Discovery, Kumamoto University）

1P-43 Synthesis of proline-type fullerene derivatives with pyridine side chain for anti HIV drugs Takumi Yasuno1*, Kyoko Takahashi1, Tomoyuki Ohe1, Shigeo Nakamura2, Tadahiko Mashino1 (1Faculty of Pharmacy, Keio University, 2Nippon Medical School)

1P-44 Synthesis and membrane attack dependent anti-MRSA activity of a series of riccardin C derivatives Kenji Onoda1*, Daichi Morita1, Hiromi Sawada1, Erika Ishitubo2, Kenji Matsuno1, Hiroaki Tokiwa2, Teruo Kuroda1, Hiroyuki Miyachi1 (1Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 2Graduate School of Science, Rikkyo University)

1P-45 Theoretical drug design and development of novel Dengue virus inhibitors Ayumi Sando1*, Karl N Kirschner2, Kazuya Hidari3, Kiyoshi Ikeda4, Hiroaki Tokiwa1,5 (1Fasility of Science, Rikkyo University, 2Fraunhofer SCAI, 3Aizu University, 4Fasirity of Pharmaceutical Science, Hiroshima International University, 5Rikkyo University, Research Center for Smart Molecules )

1P-46 Discovery of CPZEN-45, as a promising drug candidate for treating extremely drug-resistant tuberculosis (XDR-TB)

Kazushige Sasaki1*, Yoshiaki Takahashi1, Yoshimasa Ishizaki2, Masayuki Igarashi2, Toshiaki Miyake1, Masaji Okada3, Norio Doi4, Yuzuru Akamatsu2, Akio Nomoto2 (1Institute of Microbial Chemistry (BIKAKEN) Hiyoshi, 2Institute of Microbial Chemistry (BIKAKEN), 3NHO Kinki-chuo Chest Medical Center, 4Research Institute of Tuberculosis)

1P-47 Development of dipeptide-type SARS-CoV 3CL protease inhibitors Yoshio Hayashi1*, Pillaiyar Thanigaimalai1, Sho Konno1, Kiyohiko Nakada1, Takehito Yamamoto1, Yuji Koiwai1, Akihiro Taguchi1, Kentaro Takayama1, Fumika Yakushiji1, Kenichi Akaji2, Shen-En Chen3, Aurash Naser-Tavakolian3, Arne Schön3, Ernesto Freire3 (1Department of Medicinal Chemistry, Tokyo University of Pharmacy and Life Sciences, 2Department of Medicinal Chemistry, Kyoto Pharmaceutical University, 3Department of Biology, Johns Hopkins University )

1P-48 Synthesis of tricyclic compounds having novel GLP-1 secretory activity Daisuke Minehira1*, Naoki Toyooka2, Atsushi Kato1, Isao Adachi1 (1Department of Hospital Pharmacy, University of Toyama, 2Graduate School of Science and Technology, University of Toyama)

1P-49 Structure Activity Relationship Study on α-glucosidase inhibitor, salacinol: effect on toluic acid type substitution at 3’position Genzoh Tanabe1*, Shinya Nakamura1, Nozomi Tsutsui1, Jyunji Akaki2, Toshio Morikawa2, Kiyofumi Ninomiya2, Isao Nakanishi1, Masayuki Yoshikawa2, and Osamu Muraoka1 (1School of Pharmacy and 2Pharmaceutical Research and Technology Institute, Kinki University)

1P-50 Novel synthetic method for stavudine and 4'-subsutitued stavudine using oxidative glycosylation reaction. Hiroya Kan-no*, Takuya Uematsu, Yuichi Yoshimura, Hiroki Takahata. （Tohoku Pharmaceutical University.）

1P-51 Synthesis and structure-activity relationships of phenylacetic acid derivatives as CRTH2 antagonists Tadashi Terasaka1, Shinji Ito1*, Hiroshi Matsuda2, Yuji Takasuna1, Miki Kobayashi1, Yasuhiro Miyao1, Makoto Takeuchi1 (1Astellas Pharma Inc., 2Astellas Research Technologies Co., Ltd.)

1P-52 Potent and human/rat species-selective histamine H3 receptor antagonist OUP-186: Synthesis, pharmacological evaluation, and molecular modeling study Shinya Harusawa1*, Koichi Sawada2, Takuji Magata1, Hiroki Yoneyama1, Lisa Araki1,Yoshihide Usami1, Kouta Hatano2, Kouichi Yamamoto2, Daisuke Yamamoto3, and Atsushi Yamatodani2 (1Osaka University of Pharmaceutical Science, 2Graduate School of Allied Health Sciences, Faculty of Medicine, Osaka University, 3Osaka Medical College)

1P-53 Synthesis and structure-activity relationships of novel IDO inhibitors Miwa Fukuda1, Kenji Matsuno1, Akira Asai2, Osamu Takikawa3, Hiroyuki Miyachi1 (1Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 2Graduate School of Pharmaceutical Sciences, University of Shizuoka, 3National Institute for Longevity Sciences, National Center for Geriatrics and Gerontology)

1P-54 Synthesis and evaluation of quinazoline derivatives having anti-proliferative

activity against cancer cells Kenta Kuroiwa1*, Hirosuke Ishii2, Kenji Matsuno3, Akira Asai2, Yumiko Suzuki1 (1Faculity of science & technology, Sophia University, 2Graduate school of pharmaceutical sciences, University of Shizuoka, 3Graduate school of medhicine, dentistry, and pharmaceutical sciences, Okayama University)

1P-55 Synthesis and biological evaluation of colchicine derivatives as anticancer agents Hiroyuki Nishiyama1,3*, Masahiro Ono1, Takuya Sugimoto1, Toshio Sasai1, Naoyuki Asakawa1, Satoshi Ueno1, Yoshitaka Tominaga2, Takashi Yaegashi1, Masato Nagaoka1, Takeshi Matsuzaki1, Noriyuki Kogure3, Mariko Kitajima3, Hiromitsu Takayama3（1Yakult Central Institute for Microbiological Research, 2Pharmaceutical Division, Yakult Honsha Co., Ltd., 3Graduate School of Pharmaceutical Sciences, Chiba University）

1P-56 Synthesis of 2,3,6-Trisubstituted Indole Derivatives and Evaluation of Their Tumor Cell Growth Inhibition. Ayaka Matsui1, Takashi Nishiyama1, Choshi Tominari1, Hatae Noriyuki2, Hibino Satoshi1 (1Fukuyama University, 2Health Sciences University of Hokkaido)

1P-57 Affinity-based screening of MDM2/MDMX-p53 interaction inhibitors by chemical array technology Taro Noguchi1*, Shinya Oishi1, Kaori Honda2, Yasumitsu Kondoh2, Tamio Saito2, Tatsuhiko Kubo1, Masato Kaneda1, Hiroaki Ohno1, Hiroyuki Osada2, Nobutaka Fujii1 (1Graduate School of Pharmaceutical Sciences, Kyoto University, 2Antibiotics Laboratory, RIKEN, Japan)

1P-58 Discovery of HDAC8-selective inhibitors Yosuke Ota1*, Yukihiro Itoh1, Nobusuke Muto2, Hidehiko Nakagawa2, Naoki Miyata2, Takayoshi Suzuki1,3 (1Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 2Graduate School of Pharmaceutical Sciences, Nagoya City University, 3PRESTO, Japan Science and Technology Agency)

1P-59 Identification of a PHF8 inhibitor Takayoshi Suzuki1,2*, Hiroki Ozasa3, Yukihiro Itoh1, Koshiki Mino4, Hidehiko Nakagawa3, Tamio Mizukami4, Naoki Miyata3, (1Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 2PRESTO, Japan Science and Technology Agency, 3Graduate School of Pharmaceutical Science, Nagoya City University, 4Graduate School of Bio-Science, Nagahama Institute of Bio-Science Technology)

1P-60 Synthesis of KOR selective trimer with 1,3,5-trioxazatriquinane skeleton and its pharmacology Naohisa Wada1*, Shigeto Hirayama1, Takashi Iwai1, Toru Nemoto1, Hideaki Fujii1, Hiroshi Nagase1,2 (1Graduate School of Pharmacy, Kitasato University, 2The University of Tsukuba's International Institute for Integrative Sleep Medicine)

1P-61 Design and synthesis of opioid δ receptor agonists with oxazatricyclodecane structure and their pharmacologies Kohei Hayashida1*, Fujii Hideaki1, Shigeto Hirayama1, Takashi Iwai1, Toru Nemoto1, Junichi Sakai2, Takashi Kanda2, Eriko Nakata2, Hiroshi Nagase1,3 (1School of Pharmacy, Kitasato University, 2Nippon Chemiphar Co, Inc., 3International Institute for Integrative Sleep Medicine)

1P-62 Structure-activity Relationship of New Vitamin K2 Analogues Inducing Differentiation from Neuronal Progenitor Cells into Neurons in vitro Yoshitomo Suhara1*, Yoshihisa Hirota2, Rie Sakane1, Kimie Nakagawa2, Akimori Wada3, Toshio Okano2 (1Department of Bioscience and Engineering, Shibaura Institute of Technology, 2Department of Hygienic Sciecnes, Kobe Pharmaceutical University, 3Department of Organic Chemistry for Life Science, Kobe Pharmaceutical University)

1P-63 Aggregation inhibitors of amyloid β peptide based on a cyclo[-Lys-Leu-Val-Phe-Phe-] motif Tadamasa Arai1,2*, Daisuke Sasaki1,2, Takushi Araya1, Yuki Kobayashi1,2, Youhei Sohma1,2, Motomu Kanai1,2 (1Grad. Sch. of Pharm. Sci., The Univ. of Tokyo, 2JST-ERATO)

1P-64 Structure-activity relationship study of a chemical chaperone as a novel drug candidate for protein folding diseases Ritsue Sasaki*, Katsuhiro Okuda, Shigeru Ohta（Institute of Biomedical and Health Sciences, Hiroshima University）

1P-65 Attenuated aggregation and neurotoxicity of amyloid-β peptide based on catalytic photo-oxidation Youhei Sohma1,2*, Atsuhiko Taniguchi1,2, Daisuke Sasaki1,2, Azusa Shiohara1, Takeshi Iwatsubo1,3, Taisuke Tomita1, Motomu Kanai1,2 (1Graduate School of Pharmaceutical Sciences, The University of Tokyo, 2Japan Science and Technology Agency (JST), ERATO, 3Graduate School of Medicine, The University of Tokyo)

1P-66 Strategy and drug design approach to eliminate metabolic activation of hapatotoxic drugs: identification of novel reactive metabolites of benzbromarone and labetarol and their implications for hepatotoxicity. Tomoyuki Ohe1*, Yumina Kitagawara1, Fumiko Nakamura1, Kumiko Tachibana1, Kyoko Takahashi1, Sigeo Nakamura2, Tadahiko Mashino1 (1Faculty of Pharmacy, Keio University, 2Nippon Medical School）

1P-67 Predictability of Drug-induced hepatotoxicity using three dimentional hepatocyte culture Masashi Takagi1*, Seigo Sanoh1,2, Masataka Santoh2, Yoko Ejiri3, Kazumi Sugihara4, Toru Horie5, Sigeyuki Kitamura6, Sigeru Ohta1,2 (1Faculty of Pharmaceutical Sciences,Hiroshima University, 2Graduate School of Biomedical and Health Sciences, 3Tsukuba Research Center,Kuraray Co.,Ltd., 4Faculty of Pharmaceutical Sciences,Hiroshima International University, 5De Three Research Laboratories, 6Nihon Pharmaceutical University)

Poster Presentation Day2 (2P-01～68) 2P-01 Synthetic studies on Vitamin D derivatives with lactone and lactam structure

on side chain Rumi Abe*, Aya Hokazono, Yu Nagai, Keisuke Iida, Kazuo Nagasawa (Faculty of Enginnering, Tokyo University of Agriculture and Technology)

2P-02 Novel synthesis of bicyclic amidines by the rearrangement reaction of aminal Kenichi Murai*, Masato Shimura, Ryu Nagao, Hideyuki Komatsu, Daisuke Endo,

Hiromichi Fujioka (Graduate School of Pharmaceutical Sciences, Osaka University)

2P-03 Development of bioactive silicon-containing compounds Masaharu Nakamura*, Daisuke Kajita, Hirozumi Toyama, Yotaro Matsumoto and Yuichi Hashimoto (Institute of Molecular and Cellular Biosciences, The University of Tokyo)

2P-04 Development of functional amino acid derivatives bearing trifluoromethyl groups for the stabilization of its molecular structure Minoru Waki1*, Toshimasa Katagiri2, Kenji Matsuno1, Hiroyuki Miyachi1 (1Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 2Faculty of Engineering, Okayama university)

2P-05 Design and synthesis of opioid delta selective propellane type quinoline derivatives Ryo Nakajima1,2,3*, Naoshi Yamamoto2, Shigeto Hirayama3, Takashi Iwai3, Toru Nemoto3, Hideaki Fujii3, Horoaki Gouda3,4, Shuichi Hirono3,Hiroshi Nagase2,3 (1Graduate School of Pure and Applied Sciences University of Tsukuba, 2International institute for Integrateve Sleep Medicine, 3School of Phamacy Kitasato University,4School of Phamacy Showa University)

2P-06 Synthetic studies of centromere-associated protein-E (CENP-E) inhibitors: Exploration of fused bicyclic core scaffolds using electrostatic potential map Takaharu Hirayama*, Masanori Okaniwa, Takashi Imada, Akihiro Ohashi, Momoko Ohori, Kenichi Iwai, Kouji Mori, Tomohiro Kawamoto, Akihiro Yokota, Toshimasa Tanaka, and Tomoyasu Ishikawa (Takeda Pharmaceutical Company, Ltd.)

2P-07 Microwave-assisted continuous-flow organic synthesis: Some examples of microwave effects Saori Yokozawa1*, Noriyuki Ohneda1, Ken Muramatsu1, Takashi Ikawa2, Jun-ichi Sugiyama3, Tadashi Okamoto1, Masahiro Egi4, Yoshitaka Hamashima4, Shuji Akai2 (1SAIDA FDS INC., 2Graduate School of Pharmaceutical Sciences, Osaka University, 3AIST, 4School of Pharmaceutical Sciences, University of Shizuoka)

2P-08 Asymmetric α‑Arylation of Amino Acid Derivatives by Nucleophilic Aromatic Substitution via Memory of Chirality Keisuke Tomohara, Ryuichi Hyakutake*, Pan Yang, Tomoyuki Yoshimura, Takeo Kawabata (Institute for Chemical Research, Kyoto University)

2P-09 Efficient screening using one-dimensional Chiral TLC for method development on the column for Medium Pressure Liquid Chromatography Hajime Tanabe*, Ichiyoshi Kanai, Tatsuo Kishimoto, Isamu Ikeda, Toshiharu Minoda (DAICEL CORPORATION)

2P-10 Intramolecular asymmetric cross aldol reaction catalyzed by axially chiral catalysts with aniline type amine Tomonori Baba*, Junya Yamamoto, Takumi Furuta, Takeo Kawabata (Institute for Chemical Research, Kyoto University)

2P-11 SAR and mode of action studies of belactosin A derivatives Yuka Unno1*, Shuhei Kawamura2, Mitsuhiro Arisawa2, Akira Asai1, Satoshi Shuto2

(1University of Shizuoka, 2Hokkaido University)

2P-12 Development of Natural Product-like Library by Using Diversity-enhanced Natural Extracts Haruhisa Kikuchi,* Kazuyoshi Sakurai, Tetsuri Watanabe, Yota Nakashiro, Yoshiteru Oshima (Graduate School of Pharmaceutical Sciences, Tohoku University)

2P-13 Synthesis and biological activity of 14-epi-tachysterol derivatives and study of their binding configuration for vitamin D receptor Dasiuke Sawada1*, Yuya Tsukuda1, Kyohei Horie2, Akiko Takeuchi2, Shinji Kakuda2, Midori Takimoto-Kamimura2, Atsushi Kittaka1 (1Faculty of Pharmaceutical Sciences, Teikyo University, 2Teijin Institute for Bio-medical Research, Teijin Pharma Ltd. )

2P-14 Synthesis and Antibacterial Activity of Novel Pleuromutilin Derivatives Yoshimi Hirokawa, Maria Kitamura, Naoyoshi Maezaki (Faculty of Pharmacy, Osaka Ohtani University)

2P-15 Structure-activity Relationship Studies of Atpenin A5 Keisuke Yano*, Atsuyoshi Miyao, Masaki Ohtawa, Shiho Arima, Satoshi Omura, Tohru Nagamitsu (Graduate School of Pharmaceutical Sciences, Kitasato University)

2P-16 Structure-acitivity relationship study of 5-deoxynegmycin analogs: discovery of natural products with readthrough-promoting activity Akihiro Taguchi1*, Keisuke Hamada1, Masaya Kokate1, Masataka Shiozuka2, Kentaro Takayama1, Fumika Yakushiji1, Yoshiaki Nonomura2, Ryoichi Matsuda2, Yoshio Hayashi1 (1Department of Medicinal Chemistry, Tokyo University of Pharmacy and Life Sciences, 2Department of Life Sciences, The University of Tokyo)

2P-17 Synthesis and Aldose Reductase Inhibitory Activity of Marine Natural Products Lukianols and Their Analogues Ayana Tanaka1*, Kaoru Takamura1, Tsutomu Fukuda1, Fumito Ishibashi2, Masatomo Iwao1 (1Graduate School of Engineering, Nagasaki University, 2Graduate School of Fisheries Science and Environmental Studies, Nagasaki University)

2P-18 Rational Drug Design and Development of Novel Anti-Influenza Inhibitors Derived from Mumefural Erika Ishitsubo1*, Karl N. Kirshner2, Nongluk Sriwilaijaroen3,4, Takumi Hosozawa6, Hiromasa Yokoe6, Masayoshi Tubuki6, Yasuo Suzuki4, Hiroaki Tokiwa1,5

（1Department of Chemistry, Rikkyo University, 2Fraunhofer Institute SCAI, 3Faculty of Medicine, Thammasat University, 4Health Science Hills, Chubu University, 5Research Center for Smart Molecules,Rikkyo University, 6Institute of Medicinal Chemistry,Hoshi University）

2P-19 Discovery of Potent Mcl-1/Bcl-xL Dual Inhibitors by Using a Hybridization Strategy Based on Structural Analysis of Target Proteins Yuta Tanaka*, Katsuji Aikawa, Goushi Nishida, Misaki Homma, Satoshi Sogabe, Shigeru Igaki, Yumi Hayano, Tomoya Sameshima, Ikuo Miyahisa, Tomohiro Kawamoto, Michiko Tawada, Yumi Imai, Masakazu Inazuka, Nobuo Cho, Yasuhiro Imaeda, and Tomoyasu Ishikawa (Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd.)

2P-20 Stereoselective synthesis, X-ray crystallographic analysis and biological activity of new VDR partial agonists Kazuki Maekawa1*, Takeru Kudo1,Yusuke Watarai1, Michiyasu Ishizawa2, Hikaru Utida2, Makoto Nakabayashi2, Nobutoshi Ito3, Hiroaki Tokiwa1, Makoto Makishima2, Sachiko Yamada2（1College of Science Rikkyo University, 2Nihon University School of Medicine, 3Medical Research Institute Tokyo Medical and Dental University）

2P-21 A Novel Computational Approach to Predict Phototoxicity of Drug Candidates Shinnosuke Hayashi1*, Youhei Miyamoto1, Takumi Aoki1, Yosuke Iura2, Akihisa Maeda1, Mie kaino1, Hiroyuki Meguro1, Chisa Kuga1, Katsuhiko Iseki1 (1Toray Industries, Inc. Pharmaceutical Research Laboratories, 2Toray Industries, Inc. Bio Business Planning Dept.)

2P-22 Utilitzation of public database:Visualization of Structure activity relationship and proposal of substituent conversion using Matched Molecular Pair Analysis Keiko Kumazawa*, Shunta Sasaki, Hitomi Yuki, Teruki Honma (RIKEN)

2P-23 Design, synthesis and evaluation of a novel visible light-controllable nitric oxide donor Naoya Ieda1*, Takayoshi Suzuki2, Naoki Miyata1, Hidehiko Nakagawa1 (1Graduate School of Pharmaceutical Sciences, Nagoya City University, 2Graduate School of Medicinal Science, Kyoto Prefectural University of Medicine)

2P-24 Development of “SEAL-tag” as a chemical probe that enables selective labeling of proteins Kohei Sato, Masaya Denda, Jun Yamamoto, Ken Sakamoto, Akira Shigenaga, Youichi Sato, Aiko Yamauchi, Akira Otaka (Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences, Tokushima University)

2P-25 Effect of cyclic imide-containing hydantoin derivatives on sodium channels Nav1.1-1.3 Jun-ichi Yamaguchi1*, Hidetoshi Inagaki2, Yuka Takizawa1, Ryo Kudo1 (1Faculty of Engineering, Kanagawa Institute of Technology, 2Biomedical Research Institute, AIST)

2P-26 Design, synthesis and phyodynamic activity of water-soluble phthalocyanines Satoru Mori*, Hideyuki Yshiyama, Etsuko Tokunaga, Norio Shibata (Department of Nanopharmaceutical Science, Graduate School of Engineering, Nagoya Institute of Technology)

2P-27 Study on development of tumor hypoxia chemiluminescent imaging probe Kensuke Okuda*, Toru Ban, Tasuku Hirayama, Hideko Nagasawa (Gifu Pharmaceutical University)

2P-28 Design and Synthesis of Drugs that Reduces Side Effect of Radiotherapy Shin Aoki1*, Shinya Ariyasu2, Akinori Morita3, Akiko Sawa1, Ippei Takahashi4, Bing Wang5, Misato Hoshi1, Takatoshi Uchida6, Soichiro Ohtani6, Yoshio Hosoi7 (1Fac. Pharm. Sci. Tokyo University of Science, 2Center for Tech. against Cancer, Tokyo University of Science, 3Tokushima University, 4Hiroshima University, 5National Institute of Radiological Sciences, 6Fac. Sci. Tech. Tokyo University of Science,

7Tohoku University) 2P-29 Design and synthesis of a novel PPARγ ligand using structure-based drug

design. Yuta Tanaka1*, Masao Ohashi2, Kanae Gamou2, Beniyama Yoko2, Minoru Waki2, Kenji Matsuno2, Hiroyuki Miyachi2 (1School of Pharmaceutical Sciences, Okayama University, 2Graduate School of Dentistry and Pharmaceutical Sciences, Okayama University)

2P-30 Design and Synthesis of PPARγ Modulators Masao Ohashi1*, Kanae Gamo1, Yuta Tanaka2, Yoko Beniyama1, Minoru Waki1, Nobuyasu Matsuura3, Makoto Makishima4, Kenji Matsuno1, Masafumi, Tenta1, Jun Eguchi1, Hiroyuki Miyachi1 (1Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 2School of Pharmaceutical Sciences, Okayama University, 3Department of Life Science, Faculty of Science, Okayama University of Science, 4Division of Biochemistry, Department of Biomedical Sciences, Nihon University School of Medicine)

2P-31 Synthesis of optically active phenylpropanoic derivatives with fluorine atom as PPARδ agonists Mitsugu Bando1*, Masao Ohashi2, Kanae Gamo2, Kenji Matsuno2, Hiroyuki Miyachi2 (1School of Pharmaceutical Sciences, Okayama University, 2Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University)

2P-32 Structure-activity relationship of 4‑(4-benzoylaminophenoxy)phenol derivatives as novel androgen receptor antagonists Yuko Kazui1*, Ayumi Yamada2, Shinya Fujii2, Hiroyuki Kagechika2, Aya Tanatani1, (1Ochanomizu University, 2Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University)

2P-33 Discovery of Selective Androgen Receptor Modulator (SARM) for the Treatment of Osteoporosis Naoya Nagata1*, Kazuyuki Furuya1, Nao Oguro1, Kentaro Kawai1, Noriko Yamamoto1, Hiroaki Nejishima1, Yuki Ohyabu1, Masahiro Satsukawa1, Isao Nakanishi2, Kiyoshi Inoguchi1, Motonori Miyakawa1 (1Kaken Pharmaceutical Co., Ltd., 2Kinki University, Department of Pharmaceutical Sicneces)

2P-34 Characterization of trialylsilyl and trialkylgermyl groups as hydrophobic phamacophores Shinya Fujii*, Yu Miyajima, Hiroyuki Masuno, Hiroyuki Kagechika (Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University)

2P-35 Discovery of novel antagonists for proton-sensing receptor GPR4 and their pharmacological activities Nobumasa Otsubo*, Takeshi Kuboyama, Jun Saito, Mayumi Saki, Jun Ouchi, Hiromasa Miyaji, Hiromi Nonaka-Kase, Yuzuru Abe, Katsutoshi Sasaki, Hidenori Takada, Junko Ushiki, Motoya Mie, Naoko Hiura, Toru Amano, Kazuaki Inoue, Haruhiko Manabe, Akihiko Watanabe, Hitoshi Arai, Kyoichiro Iida (Kyowa Hakko Kirin Co., Ltd.)

2P-36 Improvement of Aqueous Solubility of KSP Inhibitors by Modification of Ring-fused Scaffolds

Tomoki Takeuchi1*, Shinya Oishi1, Masato Kaneda1, Hiroaki Ohno1, Shinya Nakamura2, Isao Nakanishi2, Masayoshi Yamane3, Jun-ichi Sawada3, Akira Asai3,

Nobutaka Fujii1 (1Graduate School of Pharmaceutical Sciences, Kyoto University, 2Faculty of Pharmacy, Kinki University, 3Graduate School of Pharmaceutical Sciences, University of Shizuoka)

2P-37 Gαi2/Gαi3-Biased S1P1 Receptor Agonist Satoshi Yoshida*, Tomohisa Ninomiya, Satomi Sugimoto, Toshiaki Mase (Meiji Seika Pharma Co. Ltd.)

2P-38 Effect of zinc finger protein inhibitor on NF-κB signaling molecules Ryoko Koga1*, Tomohiko Ejima2, Yosuke Kanemaru2, Yuu Taguchi3, Yuri Shibata3, Jun-ichiro Inoue3, Masami Otsuka1, Mikako Fujita2（1Faculty of Life Sciences, Kumamoto University, 2School of Pharmacy, Kumamoto University, 3The Institute of Medical Science, The University of Tokyo）

2P-39 Design, synthesis and evaluation of novel HIV-1 inhibitors aiming at virus uncoating Masahiro Kamo1*, Yoshinari Okamoto2, Masami Otsuka2, Mikako Fujita3 (1School of Pharmacy, Kumamoto University, 2Faculty of Life Sciences, Kumamoto University, 3Research Institute for Drug Discovery, School of Pharmacy, Kumamoto University)

2P-40 Structure-activity relationship study of phenylpyrazole derivatives as a novel class of anti-HIV agents Shiho Okazaki1*, Tsukasa Mizuhara1, Takayuki Kato2, Atsushi Hirai2, Hideki Kurihara2, Yasuhiro Shimada2, Masahiko Taniguchi2, Hideki Maeta2, Hiroaki Togami3, Kazuya Shimura3, Masao Matsuoka3, Tomoki Takeuchi1, Hiroaki Ohno1, Shinya Oishi1, Nobutaka Fujii1 (1Graduate School of Pharmaceutical Sciences, Kyoto University, 2FUJIFILM Corporation, 3Institute for Virus Research, Kyoto University )

2P-41 Anti-MRSA activity of bis(bibenzyl) derivatives and synthesis of probes for target identification Hiromi Sawada1*, Morita Daichi1, Kenji Onoda1, Erika Ishitsubo2, Kenji Matsuno1, Hiroaki Tokiwa2, Teruo Kuroda1, Hiroyuki Miyachi1 (1Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 2Graduate School ofchemistry, Rikkyo University)

2P-42 Synthetic study on novel dengue fever virus infection inhibitor Fumiteru Teraoka1*, Tomoko Abe2, Kazuya Hidari3, Takashi Suzuki2, Tadamune Otsubo1, Kiyoshi Ikeda1 (1Faculty of Pharmaceutical Sciences. Hiroshima International University, 2Faculty of Pharmaceutical Science, University of Shizuoka, 3Department of Food and Nutrition, Junior College Division,University of Aizu)

2P-43 Development of Potent Antimalarial Compounds Designed Based on Affinity to Heme Yosuke Sakata, Yuko Kobayashi, Nobuki Kato, Naoki Umezawa, Tsunehiko Higuchi* (Graduate School of Pharmaceutical Sciences, Nagoya City University)

2P-44 Discovery of a new aminoglycoside antibiotic 2-hydroxyarbekacin (2-OH-ABK) with reduced nephrotoxicity Eijiro Umemura1*, Yoshiaki Takahashi1, Yoshihiko Kobayashi2, Kazushige Sasaki1, Minoru Yonezawa2, Toshiaki Miyake1 (1Inst. Microbial Chemistry (BIKAKEN) Hiyoshi, 2Inst. Microbial Chemistry (BIKAKEN))

2P-45 Discovery of Novel Chymase Inhibitors - Drug Design for overcoming species difference besed on SBDD – Jun Takeuchi*, Takayuki Inukai, Kenya Ochi, Shingo Nakatani, Hiroshi Kohno, Hideomi Kijima, Takashi Kondo, Tetsuya Sekiguchi, Akira Ohhata, Ryoka Miwa, Kazuhide Masago, Hiromu Egashira, Masakuni Kurono, Masaru Sakai, Akira Imagawa, Takuya Seko (ONO Pharmaceutical Co. Ltd.)

2P-46 Stereochemistry of N-sulfonyl- and N-acyl-derivatives of 1,5-benzodiazepine and the related 7-membered-ring heterocycles as vasopressin receptor antagonists. Tetsuya Yoneda1*, Jun Nakagomi1, Tomohiko Tasaka2, Hidetsugu Tabata1, Tetsuta Oshitari1, Hideyo Takahashi1, Hideaki Natsugari1 (1Teikyo University, 2Affinity Science Corporation)

2P-47 Structure based design and synthesis of heart-type fatty acid-binding protein (FABP3) inhibitors Yoko Beniyama*, Kenji Matsuno, Hiroyuki Miyachi (Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University)

2P-48 Discovery of An Orally Potent Glucokinase Activator With Mitigated CYP2C9 Liability Keisuke Maki, Masahiko Hayakawa, Mitsuaki Okumura, Takahiro Nigawara, Yohsuke Hagiwara, Nobuaki Amino, Masamichi Yuda, Susumu Igarashi (Astellas Pharma Inc.)

2P-49 The effects of new 5-isoquinolinesulfonamide-type ROCK inhibitors for intraocular pressure reduction and retinal neuroprotection in animal models Kengo Sumi1*, Yoshihiro Inoue1, Masahiro Nishio2, Yasuhito Naito3, Takamitsu Hosoya4, Masaaki Suzuki5, Hiroyoshi Hidaka1 (1R&D Laboratory, D. Western Therapeutics Institute, Inc., 2Department of Sustainable Resource Science, Graduate School of Bioresources, Mie University, 3Department of Pharmacology, School of Pharmaceutical Science, Kitasato University, 4Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 5RIKEN Center for Molecular Imaging Science)

2P-50 Design and Synthesis of Novel Tricyclic JAK inhibitors Shohei Shirakami, Hiroaki Yamasghi*, Yutaka Nakajima, Jun Maeda, Hiroaki Tominaga, Fumie Takahashi, Akira Tanaka, Koichiro Mukoyoshi, Hisao Hamaguchi, Hiroyuki Usuda, Keiko Hatanaka, Ayako Moritomo, Takeshi Hondo, Masamichi Inami, Yasuyuki Higashi, Takayuki Inoue (Astellas Pharma, Inc.)

2P-51 Isoquinoline derivatives as potent CRTH2 antagonists: Lead generation, optimization and pharmacological effects of the potent CRTH2 antagonist R. Nishikwa-Shimono, Y. Sekiguchi, T. Koami, M. Kawamura, D. Wakasugi, M. Kawanishi, K. Watanabe, Y. Asakura, A. Takaoka, S. Yamanobe, T. Takayama (Taisho Pharmaceutical Co., Ltd.)

2P-52 Synthetic studies on orally active VLA-4 antagonists for the treatment of asthma Masaki Setoguchi*, Shin Iimura, Yuuichi Sugimoto, Yoshiyuki Yoneda, Jun Chiba, Toshiyuki Watanabe, Humihito Muro, Atsushi Nakayama, Nobuo Machinaga (Daiichi Sankyo Co., Ltd.)

2P-53 Development of new anticancer drugs with cell-cycle arresting action at

M-phase Takashi Ohshima*, Bei Liu, Nisha Pang, Hiroyuki Morimoto, Yuka Iwasaki, Makoto Ohira, chika Tanaka, Yasutaka Kuroki, Tatsuhiko Kitamura, Naoki Matsuo, Kazumasa Yoshida, Nozomi Sugimoto, Masatoshi Fujita (Graduate School of Pharmaceutical Sciences, Kyushu University)

2P-54 Synthesis calothrixin B derivatives with potent antiproliferative activity Noriyuki Hatae1*, Takumi Abe1, Takashi Nishiyama2, Tominari Choshi2, Satoshi Hibino2, Chiaki Okada1, Minoru Ishikura1, Eiko Toyota1 (1School of Pharmaceutical Sciences, Health Sciences University of Hokkaido, 2Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University)

2P-55 Structure activity relationship analysis of low morecular anti-tumor compounds disrupting the p53-mdmx interaction. Saki Matsue1*, Akinori Kozatani1, Yoshihiro Matsuura1, Suzuho Takemoto1, Yasuo Nagaoka1, Masato Enari2, Shinichi Uesato1 (1Department of Life Science and Biotechnology, Kansai University, 2Division of Refractory Cancer Research, National Cancer Center Research Institute)

2P-56 Construction of chemical library system and its application for discovery of hypoxia-targeting anticancer agents. Naohisa Ogo1*, Yuka Unno1, Mai Oba2, Momomi Tsugane3, Ryuta Yamazaki3, Akira Asai1 (1Graduate School of Pharmaceutical Seiences, University of Shizuoka, 2Shizuoka Institute of Environment and Hygiene, 3Yakult Central Institute, Yakult Honsha Co., Ltd.)

2P-57 Exploring histone methyltransferase inhibitors: Structure–activity relationship studies on chaetocin Shinya Fujishiro1, Joaquin Barjau1, Eriko Iwasa1,2, Yuou Teng1,2, Yoshihiro Sohtome1*, Kousuke Dodo1,2, Yoshitaka Hamashima3, Akihiro Ito1, Minoru Yoshida1, Mikiko Sodeoka1,2 (1RIKEN, 2JST-ERATO, 3 School of Pharmaceutical Sciences, University of Shizuoka)

2P-58 Synthetic small molecules dropping off an inhibitor at lysine-specific histone demethylase 1 Yukihiro Itoh1*, Daisuke Ogasawara1,2, Koshiki Mino3, Hidehiko Nakagawa2, Noriko Sugino4, Masahiro Kawahara4, Akifumi Takaori-Kondo4, Tamio Mizukami3, Naoki Miyata2, Takayoshi Suzuki1,5 (1Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 2Graduate School of Pharmaceutical Science, Nagoya City University, 3Graduate School of Bio-Science, Nagahama Institute of Bio-Science Technology, 4Graduate School of Medicine, Kyoto University, 5PRESTO, Japan Science and Technology Agency)

2P-59 Structure activity relationship of a δ opioid receptor agonist, KNT-127 derivatives Toru Nemoto1*, Yoshihiro Ida1, Shigeto Hirayama1, Takashi iwai1, Hideaki Fujii1, Hiroshi Nagase2 (1School of Pharmacy, Kitasato University, 2International Institute for Integrative Sleep Medicine, University of Tsukuba)

2P-60 Derivatizaion from naltrexone toward mesembrane structure aiming to obtain novel opioid ligands Kazuya Konoura1*, Satomi Imaide1, Shigeto Hirayama1, Hideaki Fujii1, Hiroshi Nagase1,2 (1Graduate School of pharmacy, Kitasato University, 2The University of

Tsukuba's International Institute for Integrative Sleep Medicine） 2P-61 Discovery of a novel mGluR5 negative allosteric modulators

Tomofumi Ohyama*, Yoshitaka Numajiri, Keita Yoshikawa, Takashi Nagahara, Satoshi Kurosawa, Mitsuhiro Konno, Kazumi Nishimura, Ryoji Hayashi (Pharmaceutical Research Laboratories, Toray Industries, Inc.)

2P-62 Development of Novel Diketopiperazine-Type Anti-Microtubule Agents with Pyridine and Benzophenone Structure Yoshiki Hayashi1*, Haruka Takeno1, Yuki Shinozaki1, Takumi Chinen2, Akihiro Taguchi1, Kentaro Takayama1, Fumika Yakushiji1, Takeo Usui2, Yoshio Hayashi1 (1Department of Medicinal Chemistry, Tokyo University of Pharmacy and Life Sciences, 2Graduate School of Life and Environmental Sciences, University of Tsukuba)

2P-63 SAR study of 2,6-pyridinedicarboxylic-type BACE1 inhibitors Yoshio Hamada* (Kobe Gakuin University, Faculty of Pharmaceutical Sciences)

2P-64 Synthesis of pregabalin and fluorinated GABA derivatives Yoshiteru Tanikawa*, Ayano Sato , Ayano Kawasaki (Institute of Medicinal Chemistry, Hoshi University )

2P-65 Synthesis and evaluation of hydroxymethylcarbonyl- and hydroxyethylamine-type BACE1 inhibitors Kazuya Kobayashi1*, Tomomi Akiyama1, Yukie Nohara1, Saki Goto1, Mami Okabe1, Natsumi Sato1, Miki Itoh1, Kanami Ueno1, Yasunao Hattori1, Kenta Teruya2, Akira Sanjoh3, Atsushi Nakagawa4, Eiki Yamashita4, Kenichi Akaji1 (1Department of Medicinal Chemistry, Kyoto Pharmaceutical University, 2Department of Medicinal Chemistry, Kyoto Prefectural University of Medicine, 3R&D Center, Protein Wave Co., 4Institute for Protein Research, Osaka University)

2P-66 Discovery of orally-active GSK-3β inhibitors for Alzheimer’s disease with low lipophilicity Kazuki Nakayama*, Kenji Fukunaga, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Hiroshi Tanaka, Shinji Sunada, Mika Nabeno, Ken-ichi Saito, Jun-ichi Eguchi, Akiko Mori, Shinji Tanaka, and Takashi Horikawa (Research Division, Mitsubishi Tanabe Pharma Corporation)

2P-67 C-Terminal derivatives of ß-amyloid for the chemoprevention of Alzheimer's disease Takuya Arai1, Akiko Ohno2, Naoki Miyata1, Masaaki Kurihara2, Hidehiko Nakagawa1, Kiyoshi Fukuhara3 (1Nagoya City University, 2National Institute of Health Sciences, 3Showa University)

2P-68 New bioactive triterpenoids derivatives from African mistletoe Globemituladinklagei (Engler) Van Tieghem and Tapinanthusbangwensis (Engl. et K. krause) Denser PierreMkounga1,2*, BlandineMarlyse Ouahouo1, Hayato Ishikawa2, Gabriele Sass3, Hiroshi Nishino2, and AugustinEphrem Nkengfack1 (1Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Cameroon, 2Graduate School of Sciences and technology, Kumamoto University, Japan, 3Institute of Experimental Immunology and Hepatology University Medical Center Hamburg-Eppendorf, Germany)