title: Synthesis and cytotoxic evaluation of thiourea and N-bis-benzothiazole derivatives: a novel class of cytotoxic agents.
abstract: Benzothiazolyl thiocarbamides has been achieved using a catalytic amount of 4-dimethylaminopyridine (DMAP) followed by its chemoselective oxidative cyclization with 1,3-di-n-butylimidazolium tribromide[bbim][Br(3)] to afford the N-bis-benzothiazole derivatives. All the synthesized compounds were evaluated for cytotoxic activity against two human monocytic cell lines (U 937, THP-1) and a mouse melanoma cell line (B16-F10). Based on their IC(50) values, the majority of the benzothiazolyl thiocarbamides and N-bis-benzothiazoles had significant antiproliferative activity on U 937 and B16-F10 cells, the compounds 3b, 3e, 3f, 3k, 6c and 6h were found to be the most active. The present findings indicate clearly that the compound 3e exhibited more antiproliferative activity on U 937 cells than the standard molecule, etoposide. Nevertheless, these compounds have shown comparatively less cytotoxicity towards THP-1 cells.
authors: Fluoroorganic Division, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500607, India. kumbhare@iict.res.in
authors: Ravindra M
authors: RM
authors: Kumbhare
authors: Tulshiram
authors: T
authors: Dadmal
authors: Umesh
authors: U
authors: Kosurkar
authors: V
authors: V
authors: Sridhar
authors: J Venkateswara
authors: JV
authors: Rao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry; D002384:Catalysis; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008546:Melanoma, Experimental / Q000378:metabolism; D051379:Mice; D008956:Models, Chemical; D015394:Molecular Structure; D013890:Thiourea / Q000737:chemistry*; D020298:U937 Cells
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles; D013890:Thiourea