Synthesis, Characterization, and Anticancer Screening of SomeNew Bithiazole Derivatives

Twenty new bithiazole derivatives were synthesized by condensation of 2-{2-[(1-arylethylidene)hydrazinylidene]thiazolidin-4-ylidene}hydrazine-1-carbothioamides with halo ketones, halo esters, and α-keto hydrazonoyl halides. The structures of all prepared compounds were proposed on the basis of their IR,1H and 13C NMR, and mass spectra. All the synthesized compounds were screened for their cytotoxicity against three human cancer cell lines, HCT-116 (human colorectal carcinoma), MCF-7 (human breast adenocarcinoma), and HepG2 (human hepatocellular carcinoma). Two compounds (12d and 12b) had significantly more potent anticancer activity on HCT-116 human colorectal carcinoma cells. In the case of MCF-7 human breast cancer cells, three compounds (12b, 4b and 4a) were significantly more potent than the reference drug doxorubicin. Nine of the synthesized compounds (8a, 7a, 9b, 12d, 12c, 7b, 10a, 5a and 12b) showed a significantly higher activity than that of doxorubicin against HepG2 human liver cancer cells.