Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity

…, RJ Schmidt, HN Weller, ML Andahazy…

Index: Leftheris, Katerina; Kline, Toni; Vite, Gregory D.; Cho, Young H.; Bhide, Rajeev S.; Patel, Dinesh V.; Patel, Manorama M.; Schmidt, Robert J.; Weller, Harold N.; Andahazy, Mary L.; Carboni, Joan M.; Gullo-Brown, Johnni L.; Lee, Francis Y. F.; Ricca, Carol; Rose, William C.; Yan, Ning; Barbacid, Mariano; Hunt, John T.; Meyers, Chester A.; Seizinger, Bernd R.; Zahler, Robert; Manne, Veeraswamy Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 224 - 236

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Citation Number: 81

Abstract

Analogs of CVFM (a known nonsubstrate farnesyltransferase (FT) inhibitor derived from a CA1A2X sequence where C is cysteine, A is an aliphatic residue, and X is any residue) were prepared where phenylalanine was replaced by (Z)-dehydrophenylalanine, 2-aminoindan-2- carboxylate, 1, 2, 3, 4-tetrahydroisoquinoline-3-carboxylate (Tic), and indoline-2- carboxylate. The greatest improvement in FT inhibitory potency was observed for the Tic ...