A new series of thiazoles substituted on the chromene scaffold were prepared by facial approaches starting from (E)-1-(2,3-Dihydrochromen-4-ylidene)thiosemicarbazide derivatives (2a,b), The thiosemicarbazides (2a,b) were reacted with a series of α-halo carbonyl compounds to give the corresponding rhodanine analogues and reacted also with C-acetyl-or C-ethoxy-N-hydrazothiosemicarbazidenoyl chlorides to afford the corresponding tri- and tetra-substituted hybrid hydrazinyl thiazole substituted chromenes. The newly synthesized compounds were screened for their in-vitro antimicrobial and antitumor activities. Two of the newly synthesized compounds revealed significant antimicrobial activities against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeuroginosa, and Candida albicans. All of the tested compounds exhibited excellent anticancer activity against HCT116 (colorectal carcinoma) human cell line.
Keywords: Thiosemicarbazide, Chromene scaffold, Hydrazonoyl chlorides, Antimicrobial activity, HCT116 (colorectal carcinoma)
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