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  • Title: An efficient synthesis and biological study of novel indolyl-1,3,4-oxadiazoles as potent anticancer agents.
    Author: Kumar D, Sundaree S, Johnson EO, Shah K.
    Journal: Bioorg Med Chem Lett; 2009 Aug 01; 19(15):4492-4. PubMed ID: 19559607.
    Abstract:
    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 solvent-free 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) approximately 1microM) and selectivity against human cancer cell lines.
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