Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors

被引：31

作者：

Suchaud, Virginie

Gavara, Laurent

Saugues, Emmanuelle

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 | 2013年 / 21卷 / 14期

关键词：

Pyrazolocarbazoles; Kinase inhibitors; Pim kinases; In vitro antiproliferative activities; VITRO ANTIPROLIFERATIVE ACTIVITIES; UCSF CHIMERA; BIOLOGICAL-ACTIVITIES; DESIGN; DERIVATIVES; DISCOVERY; POTENCIES; CARBAZOLE; THERAPY; SYSTEM;

D O I：

10.1016/j.bmc.2013.05.011

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：

New 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles were prepared and evaluated for their Pim kinase inhibitory potencies as well as their antiproliferative activities toward two prostatic cancer cell lines. Pyrazolocarbazole 15a was found to be a potent Pim kinase modulator with inhibitory potency toward the three isoforms. Compound 6c strongly inhibited Pim-3 with weaker effect toward Pim-1 and Pim-2, and thus could be used as an interesting molecular tool to study Pim-3 biological functions. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：4102 / 4111

页数：10

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