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Sci. Pharm. 2015, 83(1), 27-39; doi:10.3797/scipharm.1409-14

Synthesis, Characterization, and Cytotoxicity of Some New 5-Aminopyrazole and Pyrazolo[1,5-a]pyrimidine Derivatives

Department of Organometallic and Organometalloid Chemistry, National Research Centre, El-Buhoth St, Cairo, Doki, Egypt
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Author to whom correspondence should be addressed.
Received: 23 September 2014 / Accepted: 24 October 2014 / Published: 24 October 2014
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Abstract

5-Amino-N-aryl-3-[(4-methoxyphenyl)amino]-1H-pyrazole-4-carboxamides 4a–c were synthesized by the reaction of N-(aryl)-2-cyano-3-[(4-methoxyphenyl)-amino]-3-(methylthio)acrylamides 3a–c with hydrazine hydrate in ethanol. The reaction of 5-amino-N-aryl-1H-pyrazoles 4a–c with acetylacetone 5 or 2-(4-methoxybenzylidene)malononitrile 8 yielded the pyrazolo[1,5-a]pyrimidine derivatives 7a–c and 10a–c, respectively. The structures of the synthesized compounds were established based on elemental analysis and spectral data (IR, MS, 1H-NMR, and 13C-NMR). Representative examples of the new synthesized products were screened for their in vitro cytotoxic activity against Ehrlich Ascites Carcinoma (EAC) cells.
Keywords: N-Substituted cyanoacetamide; Ketene N,S-acetals; Pyrazolo[1,5-a]pyrimidines; 5-Aminopyrazoles; Cytotoxic activity N-Substituted cyanoacetamide; Ketene N,S-acetals; Pyrazolo[1,5-a]pyrimidines; 5-Aminopyrazoles; Cytotoxic activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

HASSAN, A.S.; HAFEZ, T.S.; OSMAN, S.A. Synthesis, Characterization, and Cytotoxicity of Some New 5-Aminopyrazole and Pyrazolo[1,5-a]pyrimidine Derivatives. Sci. Pharm. 2015, 83, 27-39.

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