Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives

Turk J Pharm Sci. 2018 Dec;15(3):304-308. doi: 10.4274/tjps.64935. Epub 2018 Nov 20.

Abstract

Objectives: Urea and carbohydrazide derivatives are important compounds exhibiting cytotoxic activities. In this study, a series of new urea and carbohydrazide derivatives containing an pyridine ring were synthesized and evaluated for cytotoxic activity.

Materials and methods: The proposed structures of the synthesized compounds were confirmed using elemental analysis, IR, and 1H-NMR spectroscopic techniques. The cytotoxic potencies of synthesized compounds were determined using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay (MTT) on BRCA mutant-carrying HCC1937 and Capan-1 cell lines, as well as on MCF7, HeLa, and MRC5 cells.

Results: 3a, 3b, 3c and 3d showed cytotoxic activity against all cancer cell lines.

Conclusion: Our data indicate that compounds 3a-d are more selective to cancer cells compared with nontumoral fibroblasts; however, these compounds are not more potent on HR defective cells with BRCA mutants.

Keywords: Carbohydrazide; cytotoxic activity; urea.