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2-(3′-Indolyl)-N-arylthiazole-4-carboxamides: Synthesis and evaluation of antibacterial and anticancer activities

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dc.contributor.author Kumar, Anil
dc.contributor.author Kumar, Dalip
dc.date.accessioned 2021-10-17T13:56:24Z
dc.date.available 2021-10-17T13:56:24Z
dc.date.issued 2015-10-01
dc.identifier.uri https://www.sciencedirect.com/science/article/pii/S0960894X15008240?via%3Dihub
dc.identifier.uri http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/2858
dc.description.abstract A new series of 2-(3′-indolyl)-N-arylthiazole-4-carboxamides 17a–p has been designed and synthesized. Initial reaction of readily available thioamides 15 with bromopyruvic acid under refluxing conditions produced different thiazole carboxylic acids 16 which upon coupling with arylamines by using EDCI·HCl and HOBt afforded diverse arylthiazole-4-carboxamides 17a–p in 78–87% yields. Antibacterial activity evaluation against Gram-positive and Gram-negative bacterial strains led to compounds 17i–k and 17o as potent and selectively (Gram-negative) antibacterial agents. The cytotoxicity of thiazole carboxamides 17a–p was also evaluated on a panel of human cancer cell lines. Among the tested derivatives, compounds 17i (IC50 = 8.64 μM; HEK293T) and 17l (IC50 = 3.41 μM; HeLa) were identified as the most potent analogues of the series. Preliminary mechanism of action studies of thiazole carboxamide 17i suggested that its cytotoxicity against HeLa cells involves the induction of cell death by apoptosis. en_US
dc.language.iso en en_US
dc.publisher Elsiever en_US
dc.subject Chemistry en_US
dc.subject Indoles en_US
dc.subject Thiazole carboxamides en_US
dc.subject Antibacterial en_US
dc.subject Cancer en_US
dc.subject Cytotoxicity en_US
dc.title 2-(3′-Indolyl)-N-arylthiazole-4-carboxamides: Synthesis and evaluation of antibacterial and anticancer activities en_US
dc.type Article en_US


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