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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

1
Department of Chemistry, Tongji University, Shanghai, 200092, China
2
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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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.
Keywords: antitumor activities; indolin-2-one; chloropyrrole; synthesis antitumor activities; indolin-2-one; chloropyrrole; synthesis
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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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