Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 20, Pages 7316-7326Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm100607r
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Funding
- National Health Research Institutes, National Science Council [NSC-95-2113-M-400-001-MY3]
- Department of Health, Taiwan, ROC [DOH98-TD-G-111-019, DOH98-TD-G-111-020]
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HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model.
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