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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
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Authors Affiliations
  1. 1. Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran
  4. 4. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
  5. 5. Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, Iran

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.