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Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2013 Sep 15; Vol. 21 (18), pp. 5782-93. Date of Electronic Publication: 2013 Jul 17. - Publication Year :
- 2013
-
Abstract
- Design, synthesis and anticancer activity of a series of imine-pyrazolopyrimidinones is reported for the first time. Compounds 9d, 9n and 9o in the series show encouraging in vitro anticancer activity with low micromolar IC50 values against prostate (PC3) and breast (MCF7) cancer cell lines. Some notions about structure-activity relationships and plausible mechanism of biological activity are presented.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antigens, Neoplasm chemistry
Antigens, Neoplasm metabolism
Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Binding Sites
Cell Line, Tumor
Cell Proliferation drug effects
DNA Topoisomerases, Type II chemistry
DNA Topoisomerases, Type II metabolism
DNA-Binding Proteins chemistry
DNA-Binding Proteins metabolism
Drug Design
Drug Screening Assays, Antitumor
G2 Phase Cell Cycle Checkpoints drug effects
HeLa Cells
Humans
M Phase Cell Cycle Checkpoints drug effects
MCF-7 Cells
Molecular Docking Simulation
Protein Structure, Tertiary
Pyrazoles chemical synthesis
Pyrazoles toxicity
Pyridines chemical synthesis
Pyridines toxicity
Structure-Activity Relationship
Antineoplastic Agents chemical synthesis
Imines chemistry
Pyrazoles chemistry
Pyridines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 21
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23920485
- Full Text :
- https://doi.org/10.1016/j.bmc.2013.07.016