Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity
Tomoyoshi Imaizumi, Michinori Akaiwa, Tomoaki Abe, Takahiro Nigawara, Takanori Koike, Yoshiki Satake, Kazushi Watanabe, Osamu Kaneko, Y. Amano, Kenichi Mori, Yosuke Yamanaka, Takeyuki Nagashima, Masashi Shimazaki, Kazuyuki Kuramoto
Topics & Concepts
ChemistryMoietyKRASCysteineCovalent bondBiochemistryStereochemistryPharmacologyMutationEnzymeGeneMedicineOrganic chemistryProtein Kinase Regulation and GTPase SignalingBiochemical and Molecular ResearchCancer therapeutics and mechanisms