title: A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents.
abstract: A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a-v were prepared and studied for their anticancer activity against selected human cancer cell lines. The reaction of indolylhydrazides 3a-h with a variety of aryl isothiocyanates 4 afforded the key intermediate thiosemicarbazides 5a-v, which upon treatment with acetyl chloride produced the 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a-v in good yields. Most of the synthesized compounds showed selective cytotoxicity towards human breast cancer cell line (MDA-MB-231). Of the synthesized 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles, compound 6f is the most potent towards tested cancer cell lines (IC(50) = 0.15-1.18 μM).
authors: Department of Chemistry, Birla Institute of Technology and Science, Pilani, Rajasthan 333 031, India. dalipk@bits-pilani.ac.in
authors: Dalip
authors: D
authors: Kumar
authors: N Maruthi
authors: NM
authors: Kumar
authors: Brett
authors: B
authors: Noel
authors: Kavita
authors: K
authors: Shah
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D020128:Inhibitory Concentration 50; D013830:Thiadiazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013830:Thiadiazoles