Email this article New Pyridopyrimidone Derivatives: Synthesis, Molecular Docking Studies, and Potential Anticancer Activity
- Authors: Khalifa N.M.1,2, Alkahtani H.M.3, Al-Omar M.A.1,3, Bakheit A.H.3,4
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Affiliations:
- Pharmaceutical Chemistry Department, Drug Exploration and Development Chair (DEDC), College of Pharmacy
- Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Division
- Pharmaceutical Chemistry Department, College of Pharmacy
- Chemistry Department, Faculty of Science and Technology
- Issue: Vol 89, No 8 (2019)
- Pages: 1683-1690
- Section: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/223044
- DOI: https://doi.org/10.1134/S107036321908022X
- ID: 223044
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Abstract
A new series of pyrido[2,3-d]pyrimidones incorporated pyrazoles and fused triazoles are synthesized and tested in vitro for cytotoxic effect against cancer cell lines: HePG-2, HCT-116, MCF-7, PC-3, and A-549. Their inhibition of protein kinase is assessed. The highest growth inhibitory (IC50 0.3 µM) effect is determined for one of compounds as compared with doxorubicin (IC50 0.6 µM). A modeling study is performed for approaching the compounds mode of binding and their similarity with the positive control drugs.
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About the authors
N. M. Khalifa
Pharmaceutical Chemistry Department, Drug Exploration and Development Chair (DEDC), College of Pharmacy; Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Division
Author for correspondence.
Email: nkhalifa.c@ksu.edu.sa
Saudi Arabia, Riyadh, 11451; Giza, Cairo, 12622
H. M. Alkahtani
Pharmaceutical Chemistry Department, College of Pharmacy
Email: nkhalifa.c@ksu.edu.sa
Saudi Arabia, Riyadh, 11451
M. A. Al-Omar
Pharmaceutical Chemistry Department, Drug Exploration and Development Chair (DEDC), College of Pharmacy; Pharmaceutical Chemistry Department, College of Pharmacy
Email: nkhalifa.c@ksu.edu.sa
Saudi Arabia, Riyadh, 11451; Riyadh, 11451
A. H. Bakheit
Pharmaceutical Chemistry Department, College of Pharmacy; Chemistry Department, Faculty of Science and Technology
Email: nkhalifa.c@ksu.edu.sa
Saudi Arabia, Riyadh, 11451; Khartoum
