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Design, Synthesis, and Biological Evaluation of New Series of 2-Amido-1,3,4-Thiadiazole Derivatives As Cytotoxic Agents Publisher



Almasirad A3 ; Firoozpour L1 ; Nejati M1 ; Edraki N4 ; Firuzi O4 ; Khoshneviszadeh M4 ; Mahdavi M2 ; Moghimi S2 ; Safavi M5 ; Shafiee A2 ; Foroumadi A1, 2
Authors

Source: Zeitschrift fur Naturforschung - Section B Journal of Chemical Sciences Published:2016


Abstract

A series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol- 2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.
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