Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization

…, RL Geahlen, P Verdier-Pinard, E Hamel…

文献索引：Mu; Coffing; Riese II; Geahlen; Verdier-Pinard; Hamel; Johnson; Cushman Journal of Medicinal Chemistry, 2001 , vol. 44, # 3 p. 441 - 452

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被引用次数: 50

摘要

A series of N-alkylamide analogues of the lavendustin A pharmacophore were synthesized and tested for inhibition of the epidermal growth factor receptor (EGFR) protein tyrosine kinase and the nonreceptor protein tyrosine kinase Syk. Although several compounds in the series were effective inhibitors of both kinases, it seemed questionable whether their inhibitory effects on these kinases were responsible for the cytotoxic properties observed ...