Synthesis and biological evaluation of a new series of phenothiazine-containing protein farnesyltransferase inhibitors

被引：25
作者：
Abuhaie, Cristina-Maria [1 ]
Ghinet, Alina [1 ,2 ,3 ]
Farce, Amaury [2 ,4 ]
Dubois, Joelle [5 ]
Gautret, Philippe [2 ,3 ]
Rigo, Benoit [2 ,3 ]
Belei, Dalila [1 ]
Bicu, Elena [1 ]
机构：
[1] Alexandru Ioan Cuza Univ, Dept Organ Chem, Fac Chem, Iasi 700506, Romania
[2] Univ Lille Nord France, F-59000 Lille, France
[3] UCLille, HEI, Lab Pharmacochim, EA GRIIOT 4481, F-59046 Lille, France
[4] Inst Chim Pharmaceut Albert Lespagnol, EA GRIIOT 4481, IFR114, F-59006 Lille, France
[5] CNRS, Ctr Rech Gif, Inst Chim Subst Nat, UPR 2301, F-91198 Gif Sur Yvette, France
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 59卷
关键词：
Phenothiazine; Fanesyltransferase inhibitors; Ylide; Pyridin-(1H)-ylidene; Anticancer agent; FARNESYL TRANSFERASE INHIBITORS; N-ACYLPHENOTHIAZINE; DERIVATIVES; DISCOVERY; CANCER; CHEMOTHERAPY; VALIDATION; CHEMISTRY; YLIDES; POTENT;
D O I：
10.1016/j.ejmech.2012.11.008
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC50 values of 0.7 and 0.6 mu M, respectively. (C) 2012 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：101 / 110
页数：10
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