Novel benzothiazolyl urea and thiourea derivatives with potential cytotoxic and antimicrobial activities

Abstract

A novel series of benzothiazole urea and thiourea derivatives was synthesized and evaluated for its in vitro cytotoxicity against MCF-7 breast cancer cells. The N¹-(benzothiazol-2-yl)-N³-morpholinourea 3 displayed the highest cytotoxic activity in this series. A docked pose of 3 was obtained bound to G-quadruplex of human telomere DNA active site using the Molecular Operating Environment (MOE) module. Moreover, the synthesized compounds were screened for their antimicrobial activity against Mycobacterium tuberculosis H₃₇R_v, E. coli, S. aureus and C. albicans. Again, 3 showed the best activity against M. tuberculosis H₃₇R_v while other compounds were equipotent with ampicillin against S. aureus and E. coli.

Keywords::

• Benzothiazoles
• cytotoxicity
• antimycobacterial
• antibacterial
• G-quadruplex stabilization