Products Cited in Publications Worldwide Novel Compounds Featuring a Thiophene Carboxamide Scaffold: Synthesis, Characterization and Antiproliferative Evaluation

Novel Compounds Featuring a Thiophene Carboxamide Scaffold: Synthesis, Characterization and Antiproliferative Evaluation

Mara, Bogdan-Ionuț; Mioc, Alexandra; Deveseleanu-Corici, Livia-Nicoleta; Șoica, Codruța; Cseh, Liliana

DOI:

Abstract

Thiophene derivatives are particularly attractive for application in drug development for their versatile pharmacological properties. We synthesized a series of four compounds with thiophene carboxamide as a scaffold. The structures were established based on HR-MS and 1D- and 2D-NMR. The purity of the compounds was established to be greater than 92% by thin-layer chromatography and NMR. The cytotoxic effects of the newly synthesized compounds were evaluated against the normal HaCaT cell line and A375, HT-29, and MCF-7 cancer cell lines. The cytotoxic assessment revealed that two compounds exhibit a significant cytotoxic effect on all cancer cell lines. To investigate their potential underlying mechanisms of action, several tests were performed: immunofluorescence imaging, caspase3/7 assay, mitochondrial membrane potential (JC-1) assay, and (DCFDA) assay. MB-D2 proved to be the most cytotoxic and effective in terms of caspase3/7 activation, mitochondrial depolarization and decrease in ROS production; these effects did not occur in normal HaCaT cells, revealing that MB-D2 has a high selectivity against A375 cancer cells.

Keywords

thiophene carboxamide derivatives ; toxicity assay ; anticancer

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5-Bromo-2-thiophenecarboxylic acid

A2098457311-63-997%

5-Bromo-2-thiophenecarboxylic acid

322.0/500g

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