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

被引：11

作者：

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

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, Dept Med Chem, F-27106 Val De Reuil, France

[2] Johnson & Johnson Res Dev LLC, Early Dev, Spring House, PA 19477 USA

[3] Johnson & Johnson Res Dev, Res & Early Dev Operat, B-2340 Beerse, Belgium

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 42卷 / 05期

关键词：

farnesyltransferase inhibition; tipifarnib; zarnestra; R115777; anticancer agents;

D O I：

10.1016/j.ejmech.2006.12.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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.

引用

页码：702 / 714

页数：13

共 40 条

[1]

Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma [J].