M. El-Gaby, M. M. Ghorab, Z. H. Ismail
2017
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Medicinal Chemistry Research
Abstract
The utility of 4-isothiocyanato-N-(1-phenyl-1H-pyrazol-5-yl)benzene sulfonamide 2 in the synthesis of some novel thiosemicarbazide, carbamothioate,1,3,4-thiadiazole, azomethine, thiourea, bisthiourea and imidazole derivatives is reported. The structure of the newly synthesized compounds was confirmed on the basis of analytical and spectral data. Some of the prepared compounds were evaluated for their in vitro anticancer activity against Ehrlich ascites carcinoma cells (EAC). It was found that the corresponding 2-acetyl-N-(4-(N-(1-phenyl-1H-pyrazol-5-yl) sulfamoyl)phenyl) hydrazinecarbothioamide 7 with IC50 value (2.14 µg/ml) showed better activity than doxorubicin with IC50 value (43.6 µg/ml) as reference drug.Graphical AbstractNew thiosemicarbazide,carbamothioate,1,3,4-thiadiazole, azomethine, thiourea, bisthiourea and imidazole derivatives containing pyrazole moiety have been synthesized and evaluated for their anticancer activity.