Discovery of mono- and disubstituted 1H-pyrazolo[3,4]pyrimidines and 9H-purines as catalytic inhibitors of human DNA topoisomeraseâII&#945;.

Pogorelcnik, Barbara; Brvar, Matjaz; Zegura, Bojana; Filipic, Metka; Solmajer, Tom; Perdih, Andrej

Discovery of mono- and disubstituted 1H-pyrazolo[3,4]pyrimidines and 9H-purines as catalytic inhibitors of human DNA topoisomeraseâIIα.

Pogorelcnik, Barbara; Brvar, Matjaz; Zegura, Bojana; Filipic, Metka; Solmajer, Tom; Perdih, Andrej.

Affiliation

Pogorelcnik B; National Institute of Chemistry, Hajdrihova 19, 1001 Ljubljana (Slovenia).

ChemMedChem ; 10(2): 345-59, 2015 Feb.

Article in En | MEDLINE | ID: mdl-25522133

Subject(s)

Antineoplastic Agents/chemistry; DNA-Binding Proteins/antagonists & inhibitors; Purines/chemistry; Pyrazoles/chemistry; Pyrimidines/chemistry; Topoisomerase II Inhibitors/chemistry; Antigens, Neoplasm/metabolism; Antineoplastic Agents/pharmacology; Binding Sites; Cell Survival/drug effects; DNA Gyrase/chemistry; DNA Gyrase/metabolism; DNA Topoisomerases, Type II/metabolism; DNA-Binding Proteins/metabolism; Drug Design; Drug Evaluation, Preclinical; Hep G2 Cells; Human Umbilical Vein Endothelial Cells; Humans; MCF-7 Cells; Molecular Docking Simulation; Protein Binding; Protein Structure, Tertiary; Purines/pharmacology; Pyrazoles/pharmacology; Pyrimidines/pharmacology; Structure-Activity Relationship; Surface Plasmon Resonance; Topoisomerase II Inhibitors/pharmacology

Key words

MTT assay; anticancer agents; catalytic inhibitors; human DNA topoisomeraseâIIα; virtual screening

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Full text: 1 Database: MEDLINE Main subject: Purines / Pyrazoles / Pyrimidines / DNA-Binding Proteins / Topoisomerase II Inhibitors / Antineoplastic Agents Language: En Journal: ChemMedChem Year: 2015 Type: Article

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