Synthesis and Antitumor Activity of Some Novel Pyrazole and Thienopyrimidine Derivatives

Abstract

The novel thiosemicarbazide derivative was prepared by hydrazinolysis of isothiocyanatosulfonamide with hydrazine hydrate. It was used as a starting material for the synthesis of some novel pyrazolosulphaphenazole, phthalazine, thiourea, and 1,2,4-triazolbenzenesulfonamide derivatives. Isothiocyanato sulfonamide was cyclized with sulfanyl acetic acid to furnish the novel 2-thioxothiazolidine derivative. Treatment of p-substituted sulfamoylphenyl isothiocyanate derivatives with various O-aminoesters of thiophene derivatives yielded dimethyl thiophene-carboxylate, methylthiophene carboxylate, and thienopyrimidine derivatives. Some of synthesized compounds were evaluated for one cell line. Compounds 3, 9, 15a, 15b, and 18 exhibited remarkable antitumor activity against MCF7 (breast) human cells.

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Keywords:

• Antitumor activity
• dimethyl thiophenecarboxylate
• methylthiophene carboxylate
• thienopyrimidine
• thiosemicarbazide
• 2-thioxothiazolidine