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Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties

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Author(s): Yun-Zhou Jin | Da-Xu Fu | Nan Ma | Zhan-Cheng Li | Quan-Hai Liu | Lin Xiao | Rong-Hua Zhang

Journal: Molecules
ISSN 1420-3049

Volume: 16;
Issue: 11;
Start page: 9368;
Date: 2011;
Original page

Keywords: antitumor activities | indolin-2-one | chloropyrrole | synthesis

ABSTRACT
Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4′ position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as 0.32, 0.67, 1.19 and 1.22 μM were achieved against non-small cell lung cancer (A549), oral epithelial (KB), melanoma (K111) and large cell lung cancer cell lines (NCI-H460), respectively.
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