Litcius/Paper detail

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

2022Bioorganic & Medicinal Chemistry14 citationsDOIOpen Access PDF

Topics & Concepts

ChemistryMoietyKRASCysteineCovalent bondBiochemistryStereochemistryPharmacologyMutationEnzymeGeneMedicineOrganic chemistryProtein Kinase Regulation and GTPase SignalingBiochemical and Molecular ResearchCancer therapeutics and mechanisms