1n94
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Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates
OverviewOverview
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 a series of aryl tetrahydropyridines that, incorporate substituted glycine, phenylalanine and histidine residues. The, design, synthesis, SAR and biological properties of these compounds will, be discussed.
About this StructureAbout this Structure
1N94 is a Protein complex structure of sequences from Rattus norvegicus with ZN, HFP and TIN as ligands. Full crystallographic information is available from OCA.
ReferenceReference
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives., Gwaltney SL 2nd, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62. PMID:12657282
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