Download MendeleyPyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Bryan, M.C., Burdick, D.J., Chan, B.K., Chen, Y., Clausen, S., Dotson, J., Eigenbrot, C., Elliott, R., Hanan, E.J., Heald, R., Jackson, P., La, H., Lainchbury, M., Malek, S., Mann, S.E., Purkey, H.E., Schaefer, G., Schmidt, S., Seward, E., Sideris, S., Wang, S., Yen, I., Yu, C., Heffron, T.P.(2016) ACS Med Chem Lett 7: 100-104
- PubMed: 26819674
- DOI: https://doi.org/10.1021/acsmedchemlett.5b00428
- Primary Citation of Related Structures:
5EM5, 5EM6, 5EM7, 5EM8 - PubMed Abstract:
The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with high levels of selectivity over wtEGFR and the broader kinome is described herein.
Organizational Affiliation:
Genentech , South San Francisco, California 94080, United States.
