371765-91-2Relevant academic research and scientific papers
Design, Synthesis, and Biological Activity of 4-[(4-Cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as Potent and Selective Farnesyltransferase Inhibitors
Wang, Le,Wang, Gary T.,Wang, Xilu,Tong, Yunsong,Sullivan, Gerry,Park, David,Leonard, Nicholas M.,Li, Qun,Cohen, Jerry,Gu, Wen-Zhen,Zhang, Haiying,Bauch, Joy L.,Jakob, Clarissa G.,Hutchins, Charles W.,Stoll, Vincent S.,Marsh, Kennan,Rosenberg, Saul H.,Sham, Hing L.,Lin, Nan-Horng
, p. 612 - 626 (2007/10/03)
A novel series of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles have been synthesized as selective farnesyltransferase inhibitors using structure-based design. X-ray cocrystal structures of compound 20-FTase-HFP and A313326-
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors
Li, Qun,Claiborne, Akiyo,Li, Tongmei,Hasvold, Lisa,Stoll, Vincent S.,Muchmore, Steven,Jakob, Clarissa G.,Gu, Wendy,Cohen, Jerry,Hutchins, Charles,Frost, David,Rosenberg, Saul H.,Sham, Hing L.
, p. 5367 - 5370 (2007/10/03)
As a part of our efforts to identify potent inhibitors of farnesyltransferase (FTase), modification of the structure of tipifarnib through structure-based design was undertaken by replacing the 2-quinolones with 4-quinolones and pyridones, and subsequent
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.
Farnesyltransferase inhibitors
-
, (2008/06/13)
Compounds having the formula are farnesyltransferase inhibitors. Also disclosed are methods of making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds.
Farnesyltransferase inhibitors
-
Page/Page column 10, (2010/01/31)
Compounds having the formula are farnesyltransferase inhibitors. Also disclosed are methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds.
Farnesyltransferase inhibitors
-
, (2008/06/13)
Compounds having the formula are farnesyltransferase inhibitors. Also disclosed are methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds.
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor
Lin, Nan-Horng,Wang, Le,Cohen, Jerry,Gu, Wen-Zhen,Frost, David,Zhang, Haiying,Rosenberg, Saul,Sham, Hing
, p. 3821 - 3825 (2007/10/03)
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anticancer agents. Analogues of the potent FTI, 4-[3-biphenyl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl] -1-yl-benzonitrile, were synthesized and tested in vitro for their in
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.
Pyridone-containing farnesyltransferase inhibitors: Synthesis and biological evaluation
Hasvold, Lisa A.,Wang, Weibo,Gwaltney II, Stephen L.,Rockway, Todd W.,Nelson, Lissa T. J.,Mantei, Robert A.,Fakhoury, Stephen A.,Sullivan, Gerard M.,Li, Qun,Lin, Nan-Horng,Wang, Le,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan,Bauch, Joy,Rosenberg, Saul,Sham, Hing L.
, p. 4001 - 4005 (2007/10/03)
Farnesyltransferase inhibitors (FTIs) have been developed as potential anti-cancer agents due to their efficacy in blocking malignant growth in a variety of murine models of human tumors. To that end, we have developed a series of pyridone farnesyltransferase inhibitors with potent in vitro and cellular activity. The synthesis, SAR and biological properties of these compounds will be discussed.
Aryl tetrahydropyridine inhibitors of farnesyltransferase: Bioavailable analogues with improved cellular potency
Gwaltney II, Stephen L.,O'Connor, Stephen J.,Nelson, Lissa T. J.,Sullivan, Gerard M.,Imade, Hovis,Wang, Weibo,Hasvold, Lisa,Li, Qun,Cohen, Jerome,Gu, Wen-Zhen,Tahir, Stephen K.,Bauch, Joy,Marsh, Kennan,Ng, Shi-Chung,Frost, David J.,Zhang, Haiying,Muchmore, Steve,Jakob, Clarissa G.,Stoll, Vincent,Hutchins, Charles,Rosenberg, Saul H.,Sham, Hing L.
, p. 1363 - 1366 (2007/10/03)
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered bioavail
