Synthesis, antimicrobial and in vitro antitumor activities of a series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives

Drug Design, Development and Therapy
Nizar M MhaidatQosay Al-Balas

Abstract

Three derivatives of substituted 1,2,3-thia- or 1,2,3-selenadiazole (4a-c) were prepared and characterized by different chemical techniques. These compounds were evaluated for their antimicrobial and antitumor activities. Compounds 4a (propenoxide derivative), 4b (carbaldehyde derivative), and 4c (benzene derivative) were active against the yeast-like fungi Candida albicans. Compound 4a was active against gram-negative Escherichia coli, and compound 4c was active against the gram-positive Staphylococcus aureus. For the antitumor activity, both compounds 4b and 4c were active against all tested tumor cell lines, namely, SW480, HCT116, C32, MV3, HMT3522, and MCF-7. The activity of compound 4c was greater than that of compound 4b and more than that of the reference antitumor 5-flourouracil against the SW480, HCT116, and MCF-7 tumor cell lines. In conclusion, a number of the prepared 1,2,3-thia- or 1,2,3-selenadiazole compounds showed promising antifungal, antibacterial, and in vitro antitumor activities. Further investigations are required to explore the mechanism by which active compound are inducing their cytotoxicity.

Citations

Sep 7, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qosay A Al-BalasKarem H Alzoubi
Oct 23, 2019·Journal of Medicinal Chemistry·Ana Carolina RuberteDaniel Plano

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Methods Mentioned

BETA
nuclear magnetic resonance
column chromatography
Assay

Software Mentioned

GraphPad PRISM

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