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

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

1, 1, 1, 1, 2, 2 and 1,*
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
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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