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Molecules 2011, 16(11), 9368-9385; doi:10.3390/molecules16119368

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

Department of Chemistry, Tongji University, Shanghai, 200092, China
Department of Pharmacology, Shanghai Institute of Pharmaceutical Industry, Shanghai, 200434, China
Author to whom correspondence should be addressed.
Received: 10 October 2011 / Revised: 3 November 2011 / Accepted: 3 November 2011 / Published: 8 November 2011
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: antitumor activities; indolin-2-one; chloropyrrole; synthesis antitumor activities; indolin-2-one; chloropyrrole; synthesis

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Jin, Y.-Z.; Fu, D.-X.; Ma, N.; Li, Z.-C.; Liu, Q.-H.; Xiao, L.; Zhang, R.-H. Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties. Molecules 2011, 16, 9368-9385.

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