Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles

Dalip Kumar; N Maruthi Kumar; Kuei-Hua Chang; Ritika Gupta; Kavita Shah

doi:10.1016/j.bmcl.2011.07.089

Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5897-900. doi: 10.1016/j.bmcl.2011.07.089. Epub 2011 Jul 30.

Authors

Dalip Kumar¹, N Maruthi Kumar, Kuei-Hua Chang, Ritika Gupta, Kavita Shah

Affiliation

¹ Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India. dalipk@bits-pilani.ac.in

PMID: 21873049
DOI: 10.1016/j.bmcl.2011.07.089

Abstract

A series of 3,5-bis(indolyl)-1,2,4-thiadiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-thiocarboxamide 3 with iodobenzene diacetate underwent oxidative dimerization to give 3,5-bis(indolyl)-1,2,4-thiadiazoles 4a-n. Among the synthesized bis(indoly)-1,2,4-thiadiazoles, the compound 4h with 4-chlorobenzyl and methoxy substituents showed the most potent activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Drug Design*
Drug Discovery
Drug Screening Assays, Antitumor
Female
Humans
Inhibitory Concentration 50
Male
Molecular Structure
Neoplasms / drug therapy
Structure-Activity Relationship
Thiadiazoles / chemical synthesis*
Thiadiazoles / chemistry
Thiadiazoles / pharmacology*

Substances

Antineoplastic Agents
Thiadiazoles