Synthesis of some p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles and their anticancer activity

A series of novel p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles derivatives (2a–f, 3a–f and 5–8) were synthesized by initial condensation of p-toluenesulfonylthiosemicarbazide 1 with a series of α-halogenocarbonyls in acetone or dimethylformamide (DMF)/acetone, mixture. All our synthesized compounds were submitted for further acylation reaction in the presence of acetic anhydride. The structures of newly synthesized derivatives 2a–f, 3a–f and 5–8 were confirmed by IR, 1H-NMR, EIMS spectral data and elemental analysis. Compounds 2a, 2c, 2d, 2e and 3a showed significant anticancer activities (IC50 < 10 μM) on both prostate DU-145 and hepatocarcinoma Hep-G2 cancer cell lines.

Graphical abstractA series of novel p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles derivatives (2a–f, 3a–f and 5–8) were synthesized and their cytotoxicity was evaluated against the Human prostate DU-145 and Hepatocarcinoma Hep-G2 cancer cell lines. Compounds 2a, 2c, 2d, 2e and 3a showed significant anticancer activities (IC50 < 10 μM) on both prostate DU-145 and hepatocarcinoma Hep-G2 cancer cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide