首页> Bioorganic & medicinal chemistry> Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors.

Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors.

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第一作者： Tomoyoshi,Imaizumi

第一单位： Tsukuba Research Center, Astellas Pharma Inc.; 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. Electronic address: tomoyoshi.imaizumi@astellas.com.

作者： Tomoyoshi,Imaizumi ^[1] ; Itsuro,Shimada ^[2] ; Yoshiki,Satake ^[2] ; Susumu,Yamaki ^[2] ; Takanori,Koike ^[2] ; Takahiro,Nigawara ^[2] ; Osamu,Kaneko ^[2] ; Yasushi,Amano ^[2] ; Kenichi,Mori ^[2] ; Yosuke,Yamanaka ^[2] ; Ayako,Nakayama ^[2] ; Yoshihiro,Nishizono ^[2] ; Masashi,Shimazaki ^[2] ; Takeyuki,Nagashima ^[2] ; Kazuyuki,Kuramoto ^[2]

作者单位： Tsukuba Research Center, Astellas Pharma Inc.; 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. Electronic address: tomoyoshi.imaizumi@astellas.com. ^[1] Tsukuba Research Center, Astellas Pharma Inc.; 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. ^[2]

关键词 Hydrophobic pocket KRAS G12C mutation Non-small cell lung cancer Oral activity Steric hindrance Structure-based drug design