Abstract

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.

中文翻译：

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一些新的联苯并恶唑衍生物的合成，表征和抗癌筛选

摘要

通过将2- {2-[（（1-芳基亚乙基）肼基]噻唑烷丁-4-亚基}肼-1-碳硫酰胺与卤代酮，卤代酯和α-酮基卤代甲酰卤缩合，合成了二十种新的噻唑衍生物。根据所有化合物的IR，¹ H和¹³ C NMR和质谱图，提出了所有化合物的结构。筛选所有合成的化合物对三种人类癌细胞系HCT-116（人类结直肠癌），MCF-7（人类乳腺腺癌）和HepG2（人类肝细胞癌）的细胞毒性。两种化合物（12d和12b）对HCT-116人结肠直肠癌细胞具有显着更强的抗癌活性。对于MCF-7人乳腺癌细胞，三种化合物（12b，4b和4a）的效力明显强于参考药物阿霉素。九种合成化合物（8a，7a，9b，12d，12c，7b，10a，5a和12b）显示出比阿霉素对HepG2人肝癌细胞具有显着更高的活性。