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

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. Am...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-10, Vol.21 (19), p.5897-5900
Hauptverfasser:	Kumar, Dalip, Kumar, N. Maruthi, Chang, Kuei-Hua, Gupta, Ritika, Shah, Kavita
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2,4-Thiadiazoles Anticancer agents anticarcinogenic activity Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Bisindoles Cell Line, Tumor cytotoxicity Dimerization Drug Design Drug Discovery Drug Screening Assays, Antitumor Female General aspects Humans Hypervalent iodine regents Inhibitory Concentration 50 Male Medical sciences Molecular Structure Neoplasms - drug therapy Pharmacology. Drug treatments Structure-Activity Relationship Thiadiazoles - chemical synthesis Thiadiazoles - chemistry Thiadiazoles - pharmacology
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.07.089