New Approaches for the Uses of 2-Cyanomethyl Thiazole in the Synthesis of Fused Heterocyclic Derivatives with Anti-Tumor Activities


 2-(4,5-DIHYDRO-4-oxothiazol-2-yl)acetonitrile (1) reacted with 2- .......acetylcoumarin (2) to give the 2-(4,5-dihydro-4-oxothiazol-2-yl)- 3-(2-oxo-2H-chromen-3-yl)but-2-enenitrile (3). The reactivity of the latter product towards aromatic aldehydes 4a-d, cyanomethylene reagents 6a,b, aryl diazonium salts 10a-d, was studied to give products that were evaluated against the three cancer cells namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268). Some of them have high inhibitory effect towards three cell lines and compounds 14 and 16 were found to be more active than the standard on NCI-H460 and SF-268.