Literature DB >> 12657283

Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.

Stephen L Gwaltney1, Stephen J O'Connor, Lissa T J Nelson, Gerard M Sullivan, Hovis Imade, Weibo Wang, Lisa Hasvold, Qun Li, Jerome Cohen, Wen-Zhen Gu, Stephen K Tahir, Joy Bauch, Kennan Marsh, Shi-Chung Ng, David J Frost, Haiying Zhang, Steve Muchmore, Clarissa G Jakob, Vincent Stoll, Charles Hutchins, Saul H Rosenberg, Hing L Sham.   

Abstract

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 bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.

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Year:  2003        PMID: 12657283     DOI: 10.1016/s0960-894x(03)00094-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Ethyl 1-(2-bromo-propano-yl)-4-hydr-oxy-2,6-diphenyl-1,2,5,6-tetra-hydro-pyridine-3-carboxylate.

Authors:  G Aridoss; D Gayathri; D Velmurugan; M S Kim; Yeon Tae Jeong
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-06-27

2.  Novel synthon for incorporating 1,3-dimethyl imidazolium group into molecular architecture.

Authors:  Mikhail Berezin; Samuel Achilefu
Journal:  Tetrahedron Lett       Date:  2007-02-12       Impact factor: 2.415

  2 in total

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