Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 16588-26-4, is researched, SMILESS is BrC1=C(C=CC(=C1)[N+](=O)[O-])Cl, Molecular C6H3BrClNO2Journal, Article, Research Support, U.S. Gov’t, P.H.S., Journal of Medicinal Chemistry called Design and Synthesis of Potent Nonpeptidic Farnesyltransferase Inhibitors Based on a Terphenyl Scaffold, Author is Ohkanda, Junko; Lockman, Jeffrey W.; Kothare, Mohit A.; Qian, Yimin; Blaskovich, Michelle A.; Sebti, Said M.; Hamilton, Andrew D., the main research direction is terphenylcarboxylate aminomercaptopropylamino imidazolylmethylamino preparation farnesyl transferase inhibitor.Formula: C6H3BrClNO2.
By modification of key carboxylate, hydrophobic, and zinc-binding groups projected from a sterically restricted terphenyl scaffold, a series of simple and nonpeptide mimetics of the Cys-Val-Ile-Met tetrapeptide substrate of protein farnesyltransferase (FTase) have been designed and synthesized. A crystal structure of 4-nitro-2-phenyl-3′-methoxycarbonylbiphenyl shows that the terphenyl fragment provides a large hydrophobic surface that potentially mimics the hydrophobic side chains of the three terminal residues in the tetrapeptide. 2-Phenyl-3-{N-[1-(4-cyanobenzyl)-1H-imidazol-5-yl]methyl}amino-3′-carboxylbiphenyl, in which the free thiol group was replaced with a 1-(4-cyanobenzyl)imidazole group, shows submicromolar inhibition activity against FTase in vitro and inhibits H-Ras processing in whole cells.
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