Hisashi Kawasaki
Japan Tobacco
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Publication
Featured researches published by Hisashi Kawasaki.
ACS Medicinal Chemistry Letters | 2011
Hiroyuki Abe; Shinichi Kikuchi; Kazuhide Hayakawa; Tetsuya Iida; Noboru Nagahashi; Katsuya Maeda; Johei Sakamoto; Noriaki Matsumoto; Tomoya Miura; Koji Matsumura; Noriyoshi Seki; Takashi Inaba; Hisashi Kawasaki; Takayuki Yamaguchi; Reina Kakefuda; Toyomichi Nanayama; Hironori Kurachi; Yoshikazu Hori; Takayuki Yoshida; Junya Kakegawa; Yoshihiro Watanabe; Aidan G. Gilmartin; Mark Richter; Katherine G. Moss; Sylvie Laquerre
Inhibition of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) represents a promising strategy for the discovery of a new generation of anticancer chemotherapeutics. Our synthetic efforts, beginning from the lead compound 2, were directed at improving antiproliferative activity against cancer cells as well as various drug properties. These efforts led to the discovery of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethylsulfoxide solvate (GSK1120212, JTP-74057 DMSO solvate; 1), a selective and highly potent MEK inhibitor with improved drug properties. We further confirmed that the antiproliferative activity correlates with cellular MEK inhibition and observed significant antitumor activity with daily oral dosing of 1 in a tumor xenograft model. These qualities led to the selection of 1 for clinical development.
Archive | 2005
Toshiyuki Sakai; Hisashi Kawasaki; Hiroyuki Abe; Kazuhide Hayakawa; Tetsuya Iida; Shinichi Kikuchi; Takayuki Yamaguchi; Toyomichi Nanayama; Hironori Kurachi; Masahiro Tamaru; Yoshikazu Hori; Mitsuru Takahashi; Takayuki Yoshida
Archive | 2005
Hisashi Kawasaki; Hiroyuki Abe; Kazuhide Hayakawa; Tetsuya Iida; Shinichi Kikuchi; Takayuki Yamaguchi; Toyomichi Nanayama; Hironori Kurachi; Masahiro Tamaru; Yoshikazu Hori; Mitsuru Takahashi; Takayuki Yoshida; Toshiyuki Sakai
Archive | 2002
Hiroyuki Abe; Jonathan B. Houze; Hisashi Kawasaki; Frank Kayser; Rajiv Sharma; Samuel Sperry
Journal of Medicinal Chemistry | 1996
Hidetsura Cho; Susumu Katoh; Shinsuke Sayama; Kengo Murakami; Hiroyuki Nakanishi; Yasuyuki Kajimoto; Hiroshi Ueno; Hisashi Kawasaki; Kazuo Aisaka; Itsuo Uchida
Archive | 2004
Hisashi Kawasaki; Tetsudo Kaya; Hiroto Imai; Tomoya Miura; Yukihiro Nomura; Hiroshi Chatani; Yoshifumi Ueda; Takayuki Mimura; Hiroyuki Iwamura
Archive | 2004
Tetsudo Kaya; Hisashi Kawasaki; Shizue Watanabe; Noboru Nagahashi; Noriaki Matsumoto; Yukihiro Nomura; Hiroshi Chatani; Yoshifumi Ueda; Takayuki Mimura; Hiroyuki Iwamura
Archive | 2008
Hiroyuki Abe; Kazuhide Hayakawa; Yoshikazu Hori; Tetsuya Iida; Hisashi Kawasaki; Shinichi Kikuchi; Hironori Kurachi; Toyomichi Nanayama; Toshiyuki Sakai; Mitsuru Takahashi; Masahiro Tamaru; Naoyuki Yamaguchi; Takayuki Yoshida; 豊通 七山; 宏典 倉地; 孝行 吉田; 義和 堀; 尚之 山口; 和秀 早川; 河崎 久; 昌弘 田丸; 慎一 菊池; 敏行 酒井; 博行 阿部; 哲也 飯田; 満 高橋
Archive | 2005
Hiroyuki Abe; Kazuhide Hayakawa; Yoshikazu Hori; Tetsuya Iida; Hisashi Kawasaki; Shinichi Kikuchi; Hironori Kurachi; Toyomichi Nanayama; Toshiyuki Sakai; Mitsuru Takahashi; Masahiro Tamaru; Takayuki Yamaguchi; Tomokazu Yoshida
ACS Medicinal Chemistry Letters | 2016
Satoru Noji; Noriyoshi Seki; Takaki Maeba; Takayuki Sakai; Eiichi Watanabe; Katsuya Maeda; Kyoko Fukushima; Toru Noguchi; Kazuya Ogawa; Yukiyo Toyonaga; Tamotsu Negoro; Hisashi Kawasaki; Makoto Shiozaki
