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One-pot synthesis and in-vitro anticancer evaluation of 5-(2′-indolyl)thiazoles

Article scientifique 2016 Anglais

Résumé

A series of 5-(2'-indolyl)thiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of thioamides 3 with 3-tosyloxypentane-2,4-dione 4 led to in situ formation of 5-acetylthiazole 5 which upon treatment with arylhydrazines 6 in polyphosphoric acid resulted in the formation of 5-(2'-indolyl)thiazoles 2. Among the synthesized 5-(2'-indolyl)thiazoles, compounds 2d-f, and 2h exhibited encouraging anticancer activity and also selectivity towards particular cell lines (IC50 = 10-30 μM). Further studies on the SAR of compound 2e may result in good anticancer activity.

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Vaddula, B., Tantak, M., Sadana, R., Gonzalez, M., Kumar, D. (2016). One-pot synthesis and in-vitro anticancer evaluation of 5-(2′-indolyl)thiazoles. https://doi.org/10.1038/srep23401

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Auteur(s)

Buchi Reddy Vaddula Mukund P. Tantak Rachana Sadana Michael A. Gonzalez Dalip Kumar

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