450840-79-6Relevant articles and documents
Synthesis and activity of 1-aryl-1′-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors
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.
, p. 5371 - 5376 (2007/10/03)
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 maintaining excellent cellular activity comparable to tipifarnib. The compounds are characterized as being simple, easier to make, and possess no chiral center involved.
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability
Tong, Yunsong,Lin, Nan-Horng,Wang, Le,Hasvold, Lisa,Wang, Weibo,Leonard, Nicholas,Li, Tongmei,Li, Qun,Cohen, Jerry,Gu, Wen-Zhen,Zhang, Haiying,Stoll, Vincent,Bauch, Joy,Marsh, Kennan,Rosenberg, Saul H.,Sham, Hing L.
, p. 1571 - 1574 (2007/10/03)
A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.
