Benzimidazole clubbed with triazolo-thiadiazoles and triazolo-thiadiazines: New anticancer agents

详细信息    查看全文

• 作者：Asif Husain ; ^{drasifhusain@yahoo.com} ; ^{ahusain@jamiahamdard.ac.in} ; Mohd Rashid ; M. Shaharyar ^{yarmsy@rediffmail.com} ; Anees A. Siddiqui ; Ravinesh Mishra
• 关键词：Benzimidazole ; Triazole ; Thiadiazole ; Thiadiazine ; Anticancer
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：April, 2013
• 年：2013
• 卷：62
• 期：Complete
• 页码：785-798
• 全文大小：1214 K

文摘

Two series of Benzimidazole clubbed with triazolo-thiadiazoles (5a-q, 5r, 5s and 5x-a¹) and triazolo-thiadiazines (5t-w) were synthesized with an aim to produce promising anticancer agents. In?vitro anticancer activities of synthesized compounds were investigated at the National Cancer Institute (NCI) against NCI 60 cell line panel; results showed good to remarkable broad-spectrum anticancer activity. Among them, the compound 5h (NCS: 760452, 1-(1H-benzo [d] imidazol-2-yl)-3-(6-(2,4-dichlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl) propan-1-one) exhibited significant growth inhibition with GI₅₀ values ranging from 0.20 to 2.58?¦ÌM and found superior selectivity for the leukemia cell lines and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100?¦ÌM). The 5h may possibly be used as lead compound for developing new anticancer agents.