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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Regioselective synthesis and antitumor screening of some novel N-phenylpyrazole derivatives
Bioorganic and Medicinal Chemistry, Volume 16, No. 2, Year 2008
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Description
The versatile, hitherto unreported 4-acetyl-5-methyl-1-phenyl-3-phenylcarbamoyl-1H-pyrazole (3) was prepared via the reaction of 2-(2-phenylhydrazono)-2-chloro-N-phenylacetamide with pentan-2,4-dione in the presence of sodium ethoxide. Reaction of 3 with dimethylformamide-dimethylacetal (DMF-DMA) furnished the corresponding 4-[(E)-3-(dimethylamino)acryloyl]-5-methyl-1-phenyl-3-phenylcarbamoyl-1H -pyrazole (5). The latter product underwent regioselective 1,3-dipolar cycloaddition with some nitrilimines to afford the non-isolable dihydropyrazole intermediates which then lose dimethylamine yielding the corresponding pyrazole derivatives. The preliminary screening for the antitumor activity of all newly synthesized compounds was carried out against Ehrlich Ascites Carcinoma tumor cells. © 2007 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Farag, Ahmad M.
Egypt, Giza
Faculty of Science
Mayhoub, Abdelrahman S.
Egypt, Cairo
Faculty of Pharmacy
Barakat, Saber El Sayed
Egypt, Cairo
Faculty of Pharmacy
Bayomi, Ashraf Hassan
Egypt, Cairo
Faculty of Pharmacy
Statistics
Citations: 113
Authors: 4
Affiliations: 2
Identifiers
Doi:
10.1016/j.bmc.2007.10.015
ISSN:
09680896
Research Areas
Cancer