Synthesis and activity of 1-aryl-1′-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors

…, SL Gwaltney, KW Woods, A Claiborne, X Wang…

文献索引：Li, Qun; Wang, Gary T.; Li, Tongmei; Gwaltney II, Stephen L.; Woods, Keith W.; Claiborne, Akiyo; Wang, Xilu; Gu, Wendy; Cohen, Jerry; Stoll, Vincent S.; Hutchins, Charles; Frost, David; Rosenberg, Saul H.; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 21 p. 5371 - 5376

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被引用次数: 11

摘要

A series of imidazole-containing methyl ethers (4–5) have been designed and synthesized as potent and selective farnesyltransferase inhibitors (FTIs) by transposition of the D-ring to the methyl group on the imidazole of the previously reported FTIs 3. Several compounds such as 4h and 5b demonstrate superior enzymatic activity to the current benchmark compound tipifarnib (1) with IC50 values in the lower subnanomolar range, while ...