Design, Synthesis and Biological Evaluation of Pyrido[23-d] pyrimidine derivatives as potential anticancer agents
Background: CDK2 shows a fundamental role as a controller of cell growing, which makes it as one of the goals of anticancer inhibitors. The current study participated in design (docking and binding energy), which used to select the promising proposed compounds, synthesis of novel diverse 14 pyrido[2,3-d]pyrimidine derivatives and biological studies of the prepared compounds as promising anticancer agents aiming CDK2. All the fresh generated compounds were scanned for their anticancer activity versus MCF-7 and CaCO2 and 14 compounds were found to be active. Compounds 6c and 8d displayed expressive activity with IC50 values 7.4 and 5.5 on MCF-7 respectively. The created compounds were submitted to enzyme inspection (CDK2 TK) for assigning their inhibitory activity. The initial results showed that compound 8d, which demonstrates potent inhibitory activity towards tumor development and powerful inhibitions of CDK2 TK enzyme (89% inhibition) could be utilized as a lead candidate. Method: The products were characterized by IR, 1H NMR, 13CNMR and MS. Results and Conclusion: Preliminary bioassays indicated that most of the compounds exhibited very good antitumor activity and powerful inhibitions of CDK2 TK enzyme.
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Citation : Al-Otaibi, J.S., Ibrahim, D.A., El-Gogary, T.M. (2018) Design, Synthesis and Biological Evaluation of Pyrido[23-d] pyrimidine derivatives as potential anticancer agents. Letters in Drug Design & Discovery, 15,
ISSN : 1570-1808
Peer Reviewed : Yes