Design, Synthesis and Biological Evaluation of Pyrido[2,3-d] Pyrimidine Derivatives as Potential Anticancer Agents

Title:Design, Synthesis and Biological Evaluation of Pyrido[2,3-d] Pyrimidine Derivatives as Potential Anticancer Agents

Volume: 15 Issue: 12

Author(s): Jamelah S. Al-Otaibi, Diaa A. Ibrahim*Tarek M. EL Gogary

Affiliation:

• Department of Chemistry, Faculty of Science, Jazan University, Jazan,Saudi Arabia

Keywords: Pyrido[2, 3-d] pyrimidines, CDK2 inhibitors, docking study, binding energy, anti-proliferative activity, tumor.

Abstract: Background: CDK2 shows a fundamental role as a controller of cell growing, which makes it as one of the goals of anticancer inhibitors.

Methods: 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) for assigning their inhibitory activity.

Results: The initial results showed that compound 8d, which demonstrates potent inhibitory activity towards tumor development and powerful inhibitions of CDK2 enzyme (89% inhibition) could be utilized as a lead candidate. The products were characterized by IR, 1H NMR, 13CNMR and MS.

Conclusion: Preliminary bioassays indicated that most of the compounds exhibited very good antitumor activity and powerful inhibitions of CDK2 enzyme.

Cite this article as:

Al-Otaibi S. Jamelah, Ibrahim A. Diaa*, EL Gogary M. Tarek, Design, Synthesis and Biological Evaluation of Pyrido[2,3-d] Pyrimidine Derivatives as Potential Anticancer Agents, Letters in Drug Design & Discovery 2018; 15 (12) . https://dx.doi.org/10.2174/1570180815666180219163254