Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles

被引：35

作者：

Akue-Gedu, Rufine ^{[1
,2
]}

Nauton, Lionel ^{[1
,2
]}

Thery, Vincent ^{[1
,2
]}

Bain, Jenny ^{[3
]}

Cohen, Philip ^{[3
]}

Anizon, Fabrice ^{[1
,2
]}

Moreau, Pascale ^{[1
,2
]}

机构：

[1] Univ Clermont Ferrand, Clermont Univ, SEESIB, F-63000 Clermont Ferrand, France

[2] Univ Clermont Ferrand, Photochim Mol & Macromol Lab, CNRS, SEESIB,UMR 6504, F-63177 Aubiere, France

[3] Univ Dundee, Prot Phosphorylat Unit, MRC, Coll Life Sci,Sir James Black Ctr, Dundee DD1 5EH, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 18期

关键词：

Pyrrolo[2,3-a]carbazoles; Kinase inhibitors; PIM inhibitors; In vitro antiproliferative activities; SPECIFICITY; DOCKING;

D O I：

10.1016/j.bmc.2010.07.036

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6865 / 6873

页数：9

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