Next Article in Journal
Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives
Previous Article in Journal
Stigmasterol-Based Novel Low Molecular Weight/Mass Organic Gelators
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,*
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)
Download PDF [215 KB, 18 June 2014; original version 18 June 2014]   |  

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 (CC BY 3.0).
SciFeed

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
RIS
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert