An efficient synthesis and biological study of novel indolyl-1,3,4-oxadiazoles as potent anticancer agents

作者：Kumar Dalip^*; Sundaree Swapna; Johnson Emmanuel O; Shah Kavita

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(15): 4492-4494.

DOI：10.1016/j.bmcl.2009.03.172

• 1,3,4-Oxadiazole
• Solvent-free
• Hypervalent iodine
• Anticancer agent
• Selective cytotoxicity

A facile, convenient and high yielding synthesis of a series of novel 5-(3'-indolyl)-2-(substituted)-1,3,4-oxadiazoles from readily available starting materials has been described. The key step of this protocol is oxidative cyclization of N-acylhydrazones 1 using [bis(trifluoroacetoxy)iodo]benzene under solventfree condition. The 5-(3'-indolyl)-2-(substituted)-1,3,4-oxadiazoles were screened for their in vitro anticancer activity against various human cancer cell lines. Compounds 3c, 3d and 3j exhibited potent cytotoxicity (IC(50) similar to 1 mu M) and selectivity against human cancer cell lines.

• 出版日期2009-8-1