New Pyridopyrimidone Derivatives: Synthesis, Molecular Docking Studies, and Potential Anticancer Activity

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 (IC 50 0.3...

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Bibliographic Details
Published inRussian journal of general chemistry Vol. 89; no. 8; pp. 1683 - 1690
Main Authors Khalifa, N. M., Alkahtani, H. M., Al-Omar, M. A., Bakheit, A. H.
Format Journal Article
LanguageEnglish
Published Moscow Pleiades Publishing 01.08.2019
Springer Nature
Springer
Springer Nature B.V
Subjects
Anticancer properties
Antimitotic agents
Antineoplastic agents
Chemical synthesis
Chemistry
Chemistry and Materials Science
Chemistry, Multidisciplinary
Chemistry/Food Science
Doxorubicin
Kinases
Molecular docking
Physical Sciences
Protein kinases
Science & Technology
Triazoles
cytotoxic agents
pyridopyrimidones
molecular docking
ANTITUMOR-ACTIVITY
GROWTH
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Summary: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 (IC 50 0.3 µM) effect is determined for one of compounds as compared with doxorubicin (IC 50 0.6 µM). A modeling study is performed for approaching the compounds mode of binding and their similarity with the positive control drugs.
ISSN:1070-3632
1608-3350
DOI:10.1134/S107036321908022X