A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents

作者：Kumar Dalip^*; Kumar N Maruthi; Noel Brett; Shah Kavita

来源：European Journal of Medicinal Chemistry, 2012, 55: 432-438.

DOI：10.1016/j.ejmech.2012.06.047

• 2-Arylamino-1,3,4-thiadiazoles
• Indolyl heterocycles
• Cytotoxic agents
• 1,3,4-Thiadiazoles

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 (IC50 = 0.15-1.18 mu M).

• 出版日期2012-9