Synthesis and biological evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide derivatives as lipoxygenase inhibitor with potential anticancer activity

Document Type: Research article

Authors

1 department of medicinal chemsitry, faculty of pharmacy, kermanshah university of medical sciences

2 Department of Pharmacology, Toxicology and Medical Services, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

3 Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran

4 aNovel Drug Delivery Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

Abstract

In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as novel target for discovery of anticancer drugs. PC3, HT29 and SKNMC cell lines were utilized and the obtained results were compared to doxorubicin. Overall, nitro containing derivatives exerted higher cytotoxic activity against PC3 cell line and methoxylated derivatives showed an acceptable activity against SKNMC cell line. Methoxylated derivatives were also the most potent enzyme inhibitors especially at position ortho of the phenyl residue.

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