Author(s): Kumar D, Sundaree S, Johnson EO, Shah K
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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.
This article was published in Bioorg Med Chem Lett
and referenced in Medicinal Chemistry