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Issue 25, 2015
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Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker

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Abstract

Forty-two compounds (series 8, 9 and 10) incorporated with diacylated piperazine have been synthesized and evaluated as novel Bcr-Abl inhibitors based on ‘six-atom linker’. Five of them, 8d, 8h, 8l, 10m and 10p, displayed potent Bcr-Abl inhibitory activity comparable with Imatinib. Moreover, compounds 8e, 10q, 10s, and 10u were potent Bcr-Abl inhibitors with IC50 values at the sub-micromolecular level. Most compounds exhibited moderate to high antiproliferative activity against K562 cells. In particular, compound 9e was the most promising Bcr-Abl inhibitor. Docking studies revealed that the binding modes of these compounds were similar with Imatinib. These compounds could be considered as promising lead compounds for further optimization.

Graphical abstract: Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker

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Supplementary files

Article information


Submitted
03 Mar 2015
Accepted
20 May 2015
First published
21 May 2015

Org. Biomol. Chem., 2015,13, 7050-7066
Article type
Paper
Author version available

Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker

X. Pan, J. Dong, Y. Shi, R. Shao, F. Wei, J. Wang and J. Zhang, Org. Biomol. Chem., 2015, 13, 7050
DOI: 10.1039/C5OB00430F

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