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Anticancer Activity Of 4-[1-Oxo-(Substituted Aryl)-2-Propenyl]-3-Phenylsydnones

Author(s): K Satyanarayana, S. R Deshpande, B Subba Rao, M. N. A Rao

Novel structural feature containing 4-[1-oxo-(substituted aryl)-2-propenyl]-3-phenylsydnones were synthesized and screened for anticancer activity. These compounds contain two pharmacophores,a,b unsaturated ketone moiety and sydnone nucleus. Three compounds were synthesized, and all of the three exhibited promising in vitro cytotoxicity In 56 cell lines representing cancers of non-small cell lung, colon, CNS, melanoma, ovarian, prostrate, breast and leukemia. Average growth inhibition of 50% was in the range of 1.7-3.5 μM. Methyl derivative was highly selective against SNB-75 tumor cell line of CNS. It was active at less than one nano mole. However, in vivo the activity was moderate by hollow fiber assay model.