Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors

被引：26

作者：

Gavara, Laurent

Suchaud, Virginie

Nauton, Lionel

Thery, Vincent

Anizon, Fabrice ^{[1
]}

Moreau, Pascale

机构：

[1] Univ Clermont Ferrand, Clermont Univ, Inst Chim Clermont Ferrand, F-63000 Clermont Ferrand, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 08期

关键词：

Pyrrolo[2,3-g]indazole; Indazole; Indole; Pim kinase inhibition; VITRO ANTIPROLIFERATIVE ACTIVITIES; UCSF CHIMERA; BIOLOGICAL-ACTIVITIES; DERIVATIVES; PROTEIN; INDAZOLES; DISCOVERY; POTENCIES; SYSTEM;

D O I：

10.1016/j.bmcl.2013.02.074

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and Pim kinase inhibition potency of a new series of pyrrolo[2,3-g] indazole derivatives is described. The results obtained in this preliminary structure-activity relationship study pointed out that sub-micromolar Pim-1 and Pim-3 inhibitory potencies could be obtained in this series, more particularly for compounds 10 and 20, showing that pyrrolo[2,3-g] indazole scaffold could be used for the development of new potent Pim kinase inhibitors. Molecular modeling experiments were also performed to study the binding mode of these compounds in Pim-3 ATP-binding pocket. (C) 2013 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2298 / 2301

页数：4

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