Design,synthesis and anticancer evaluation of novel pyrazole,pyrazolo[3,4-d]pyrimidine and their glycoside derivatives |
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| Authors: | Ibrahim F Nassar Ahmed F El Farargy Fathy M Abdelrazek Nasser SM Ismail |
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| Institution: | 1. Faculty of Specific Education, Ain Shams University, Abassia, Cairo, Egypt;2. Department of Chemistry, Faculty of Science, Zagazig University, Zagazig, Egypt;3. Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt;4. Pharmaceutical Chemistry Department, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University, Cairo, Egypt |
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| Abstract: | The chalcone derivatives 3a,b were cyclized upon reaction with thiourea to give the pyrazolo3,4-d]pyrimidine derivatives 5a,b. Condensation of 5a,b and their hydrazide derivatives 8a,b with cyclic and acyclic glucose gave the condensed S- and N-glycosides 7a,b and 9a,b, respectively. Reaction of 3b with ethyl cyanoacetate followed by reaction with cyclic glucose afforded a mixture of the O- and/or N-glycoside isomers 12 and 13, respectively. The pyrazolo3,4-c]pyrazole derivative 14 was also obtained from the reaction of 3b with hydrazine hydrate. A number of the synthesized compounds were screened for their antitumor activity against three different tumor cell lines HEPG2 (liver), HCT116 (colon) and MCF-7 (breast) with a docking study against CDK2. |
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| Keywords: | Pyrazole pyrazolopyrimidine cytotoxicity study molecular modeling |
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