Search for human DNA topoisomerase II poisons in the group of 2,5-disubstituted-1,3,4-thiadiazoles

Journal of Enzyme Inhibition and Medicinal Chemistry
Tomasz PlechPiotr Paneth

Abstract

A series of six 2,5-disubstituted 1,3,4-thiadiazole derivatives was synthesized and examined for cytotoxic activity in MCF-7 and MDA-MB-231 breast cancer cells. MTT assay confirmed that 2-(3-fluorophenylamino)-5-(3-hydroxyphenyl)-1,3,4-thiadiazole (2), 2-(4-bromophenylamino)-5-(2,4-dichlorophenyl)-1,3,4-thiadiazole (3), 2-(4-fluorophenylamino)-5-(2,4-dichlorophenyl)-1,3,4-thiadiazole (4), had ability to inhibit MCF-7 and MDA-MB-231 cells proliferation. The IC50 values for the mentioned compounds ranged between 120 and 160 μM (with respect to MCF-7 cells) and from 70 to 170 μM (with respect to MDA-MB-231 cells). It turned out, moreover, that compound 2 is a human topoisomerase II (topoII) catalytic inhibitor whereas the two other compounds (i.e. 3 and 4) are capable of stabilizing DNA-topoII cleavage complex and thus are topoII poisons.

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Citations

Mar 9, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Daniel SzulczykMarta Struga
Sep 24, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sara JanowskaMonika Wujec
Sep 4, 2020·Pharmacological Reports : PR·Monika Szeliga
Oct 16, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Wojciech PłonkaPiotr Paneth
Jun 6, 2018·Journal of Medicinal Chemistry·Wei HuXun Li

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