title: Synthesis, antimicrobial and in vitro antitumor activities of a series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives.
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.
authors: Department of Clinical Pharmacy, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan ; Faculty of Pharmaceutical Sciences, Hashemite University, Zarqa, Jordan.
authors: Nizar M
authors: NM
authors: Mhaidat
authors: Department of Applied Chemical Sciences, Jordan University of Science and Technology, Irbid, Jordan.
authors: Mousa
authors: M
authors: Al-Smadi
authors: Department of Applied Biological Sciences, Faculty of Science and Arts, Jordan University of Science and Technology, Irbid, Jordan.
authors: Fouad
authors: F
authors: Al-Momani
authors: Department of Clinical Pharmacy, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
authors: Karem H
authors: KH
authors: Alzoubi
authors: Faculty of Pharmaceutical Sciences, Hashemite University, Zarqa, Jordan.
authors: Iman
authors: I
authors: Mansi
authors: Department of Medicinal Chemistry and Pharmacognosy, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
authors: Qosay
authors: Q
authors: Al-Balas
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D002470:Cell Survival / Q000187:drug effects; D052978:Disk Diffusion Antimicrobial Tests; D004305:Dose-Response Relationship, Drug; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D005472:Fluorouracil / Q000494:pharmacology; D045325:HCT116 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D016566:Organoselenium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D016566:Organoselenium Compounds; D013830:Thiadiazoles; D005472:Fluorouracil
keywords: antimicrobial activity; cell lines; selenadiazole; thiadiazole