Thursday, May 4, 2017

Thiol Specific and Tracelessly Removable Bioconjugation via Michael Addition to 5-Methylene Pyrrolones

Yingqian Zhang†⊥, Xiaoping Zhou†⊥, Yonghui Xie†, Marc M. Greenberg§ , Zhen Xi†‡, and Chuanzheng Zhou

† State Key Laboratory of Elemento-Organic Chemistry and Department of Chemical Biology, College of Chemistry, Nankai University, Tianjin 300071, China
‡ Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300071, China
§ Department of Chemistry, Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218, United States

J. Am. Chem. Soc., 2017, 139 (17), 6146–6151
DOI: 10.1021/jacs.7b00670

Discovery and Characterization of Divarasib (GDC-6036), a Potent Covalent Inhibitor of KRAS G12C

Nicholas F. Endres, Steven Do, Rana Mroue, Jack A. Terrett, Matt Saabye, Angela Oh, Thomas Hunsaker, Emily Chan, John C. Tran, Lan K. Nguyen...