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“On water” expedient synthesis of 3-indolyl-3-hydroxy oxindole derivatives and their anticancer activity in vitro

Sai Prathima1, Rajesh Pamanji2, J. Venkateswara Rao2, U. Sai Kailash3, B.Sridhar4, M. Mohan Rao1*

Eur J Med Chem. 2014;84:155-9.

Inorganic & Physical Chemistry Division, Indian Institute of Chemical Technology, Hyderabad-500607, India.

Biology Division, Indian Institute of Chemical Technology, , Hyderabad-500607, India.

National Centre for Cell Sciences, Pune university campus, Pune-411007, India.

X-ray Crystallography Division, Indian Institute of Chemical Technology, Hyderabad-500607, India.

 

Abstract

Indoles are compounds having a pyrrole ring attached to benzene with broader biological relevance. In neurons indole is helpful for the synthesis of signaling molecules like serotonin that is primarily involved in control of cognitive functions, mood, apetite and sleep. Furthermore, prokaryotes like bacteria synthesize indoles for stabilizing plasmids, developing virulence and drug resistance. Of late, Indole scaffolds have emerged as potential chemo therapeutic agents against various cancers. In view of its significance, we describe a green synthetic method for novel 3-indolyl-3-hydroxy oxindole derivatives (n=41) and their anti cancer potential on various leukemic cancer cell lines (U937, THP-1), lung cancer (A549) and breast cancer cell line (MCF7). As tested, 73% of the newly synthesized compounds showed anti cancer activity with moderate to significant potential. The order of sensitivity of human cancer cell lines towards oxindole derivatives is MCF7 > U937 > A549 > THP1.Compounds 34, 36, 38 and 41 had shown effective cytotoxic activities on leukemic cell line U937. Compounds 12, 35, 40 and 41 have shown significant activity on breast cancer cell line MCF7. Notably the anti-proliferation activities of the above mentioned compounds were much better than the positive control, Etoposide. Furthermore, these derivatives could be developed as potent anti cancerous drug molecules after evaluating on other cancer cell lines and also in vivo.

Copyright © 2014 Elsevier Masson SAS. All rights reserved.

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"On water" expedient synthesis of 3-indolyl-3-hydroxy oxindole derivatives anticancer activity- global medical discovery