450840-75-2Relevant academic research and scientific papers
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.
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors
Wang, Le,Lin, Nan-Horng,Li, Qun,Henry, Rodger F.,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan C.,Bauch, Joy L.,Rosenberg, Saul H.,Sham, Hing L.
, p. 4603 - 4606 (2007/10/03)
The synthesis and biological evaluation of two novel series of potent and selective FTase inhibitors are described. Two novel series of potent and selective FTase inhibitors have been synthesized using structure-based design. Medicinal chemistry efforts led to the discovery of compound 4e with potent cellular activity and good oral bioavailability in dog. A synthetic route toward novel heterocycles 1,5-dimethyl-6-oxo-4-aryl-1,6-dihydro-pyridine-2- carbonitrile was established. The structure of compound 5c was confirmed by X-ray crystallography.
Farnesyltransferase inhibitors
-
, (2008/06/13)
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
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.
Farnesyltransferase inhibitors
-
, (2008/06/13)
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
