2007 · EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra® series

Angibaud, Patrick, Mevellec, Laurence, Meyer, Christophe, Bourdrez, Xavier, Lezouret, Patricia, Pilatte, Isabelle, Poncelet, Virginie, Roux, Bruno, Merillon, Sophie, End, David W., Van Dun, Jacky, Wouters, Walter, Venet, Marc

Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Année: 2007
Volume: 42
Numéro: 5
Pages: 702-714
Mois: MAY
DOI: 10.1016/j.ejmech.2006.12.007

Abstract

Based on the structure of R 115777 (tipifarnib, Zarnestra (R)), a series of farnesyltransferase inhibitors have been synthesized by modification of the 2-quinolinone motif and transposition of the 4-chlorophenyl ring to the imidazole or its replacement by 5-membered rings. This has yielded a novel series of potent farnesyltransferase inhibitors. (c) 2007 Elsevier Masson SAS. All rights reserved.

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