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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

Tomoyoshi Imaizumi,Itsuro Shimada,Yoshiki Satake,Susumu Yamaki,Takanori Koike,Takahiro Nigawara,Osamu Kaneko,Yasushi Amano,Kenichi Mori,Yosuke Yamanaka,Ayako Nakayama,Yoshihiro Nishizono,Masashi Shimazaki,Takeyuki Nagashima,Kazuyuki Kuramoto

Bioorganic & medicinal chemistry（2023）

Cited 0|Views9
Key words
KRAS G12C mutation,Non -small cell lung cancer,Structure -based drug design,Hydrophobic pocket,Steric hindrance,Oral activity
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