Copyright (c) 2014 AJC
This work is licensed under a Creative Commons Attribution 4.0 International License.
Synthesis and Biological Evaluation of a Benz[cd]indol-2(1H)-one Derivatives
Corresponding Author(s) : Shou-Zhi Yi
Asian Journal of Chemistry,
Vol. 26 No. 21 (2014): Vol 26 Issue 21
Abstract
Virtual screening of a library of 6.4 million compounds versus the structure of Xenopus Laevis' Aurora B kinase identified 1-(n-propyl)-6-[2-(carboxyl)tetrahydropyrrol-1-yl]sulfonyl-benzo[cd]indol-2(1H)-one 1 as a possible lead compound. Then, a novel series of benz[cd]indol-2(1H)-one derivatives were synthesized and evaluated as Aurora B kinase inhibitors. The structures of the synthetic compounds were confirmed by 1H NMR, IR, mass spectrometry and elemental analysis. These compounds were evaluated by in vitro enzyme assay using spectrophotometry. Among them, compound 7e displayed potent antitumor activity against Aurora B kinase.
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