Design, synthesis and biological evaluation of certain CDK2 inhibitors based on pyrazole and pyrazolo[1,5-a] pyrimidine scaffold with apoptotic activity

[Display omitted] •19 Compounds were screened against CDK2/cyclin A2 enzyme.•Target compounds were assessed in vitro against MCF-7, HepG2, A549 and Caco-2 tumor cell lines.•7d and 10b exhibited high anticancer activity against the four tumor cell lines.•Cell cycle colorimetric assay was performed fo...

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Veröffentlicht in:	Bioorganic chemistry 2019-05, Vol.86, p.1-14
Hauptverfasser:	Ali, Ghada M.E., Ibrahim, Diaa A., Elmetwali, Amira M., Ismail, Nasser S.M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anticancer Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis Apoptosis - drug effects CDK2 Cell cycle Cell Cycle - drug effects Cell Line, Tumor Cell Proliferation - drug effects Cyclin-Dependent Kinase 2 - antagonists & inhibitors Cyclin-Dependent Kinase 2 - metabolism Dose-Response Relationship, Drug Drug Design Drug Screening Assays, Antitumor Humans Molecular modeling Molecular Structure Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrazole Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Pyrazolo[1,5-a]pyrimidine Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Structure-Activity Relationship
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