Abdel-Rahman Hamdy M, Morsy Mohamed A
Pharmaceutical Medicinal Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
J Enzyme Inhib Med Chem. 2007 Feb;22(1):57-64. doi: 10.1080/14756360600991082.
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 H37Rv, E. coli, S. aureus and C. albicans. Again, 3 showed the best activity against M. tuberculosis H37Rv while other compounds were equipotent with ampicillin against S. aureus and E. coli.