Synthesis and biological screening of 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles as antiproliferative and anti-inflammatory agents

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• 作者：Sreevani Rapolu ; Manjula Alla ; Vittal Rao Bommena ; Ramalinga Murthy ; Nishant Jain ; Venkata Ramya Bommareddy ; Madhava Reddy Bommineni
• 关键词：Indole-3-carboxlic acids ; Indolyl-1 ; 3 ; 4-oxadiazoles ; Antiproliferative agents ; Anti-inflammatory agents
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：August, 2013
• 年：2013
• 卷：66
• 期：Complete
• 页码：91-100
• 全文大小：509 K

文摘

A series of 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles were efficiently synthesized by oxidative cyclisation of N¡ä-benzylidene-(1H-indol-3-yl)alkane hydrazides using di(acetoxy)iodobenzene. N¡ä-Benzylidene-(1H-indol-3-yl)alkane hydrazides themselves were derived from simple indole-3-carboxylic acids. The 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles were evaluated for their anti-inflammatory and anti-proliferative activities. Based on the results obtained structure and activity relationship (SAR) was established and a correlation between the activities was observed. Compound 6i and 6t showed best activity against proliferation of human cancer cell lines and as well as inflammation of rat paw edema.