Synthesis and biological evaluation of novel pyrrolopyrrolizinones as anticancer agents

被引:57
作者
Rochais, C.
Lisowski, V.
Dallemagne, P.
Rault, S.
机构
[1] Univ Caen, Ctr Etud & Rech Medicament Normandie, F-14032 Caen, France
[2] Fac Pharm Montpellier, F-34093 Montpellier 5, France
关键词
cyclization; pyrroles; fused-ring systems; L1210 murine leukemia cells;
D O I
10.1016/j.bmc.2006.09.022
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We herein describe the synthesis of novel 3-(het)aryl-pyrrolo[2,3-b]pyrrolizin-8(1H)-ones starting from commercial (het)aryl-acetonitriles. A more convergent route was also described through the first synthesis of ethyl 3-amino-4-bromo-1H-pyrrole-2-carboxylate 17. The antiproliferative activities of these compounds were tested toward various cell lines and one of them 10k shows interesting cytotoxic properties, although it was less potent than our lead compound in thiophene series 1k. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:8162 / 8175
页数:14
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