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)
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.
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.
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
