A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity

A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity

A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5H-indeno[1,2-b]pyridin-5-one (TI-1-190) was synthesized using a simple microwave-assisted method and its mode of action was systematically characterized. It is a DNA intercalative human topoisomerase IIα catalytic inhibitor with much stronger activity and les...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2017-06, Vol.53 (51), p.6864-6867
Hauptverfasser: Jeon, K H, Park, C, Kadayat, T M, Shrestha, A, Lee, E S, Kwon, Y
Format: Artikel
Sprache:eng
Schlagworte:
Anticancer properties
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Biocatalysis
Biocompatibility
Caspase 3 - metabolism
Catalysis
Catalysts
Cell Line, Tumor
Cell Proliferation - drug effects
Deoxyribonucleic acid
Derivatives
DNA Topoisomerases, Type II - metabolism
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Inhibitors
Intercalating Agents - chemical synthesis
Intercalating Agents - chemistry
Intercalating Agents - pharmacology
MCF-7 Cells
Molecular Structure
Poly-ADP-Ribose Binding Proteins - antagonists & inhibitors
Poly-ADP-Ribose Binding Proteins - metabolism
Structure-Activity Relationship
Surgical implants
Topoisomerase II Inhibitors - chemical synthesis
Topoisomerase II Inhibitors - chemistry
Topoisomerase II Inhibitors - pharmacology
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Beschreibung
Zusammenfassung:A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5H-indeno[1,2-b]pyridin-5-one (TI-1-190) was synthesized using a simple microwave-assisted method and its mode of action was systematically characterized. It is a DNA intercalative human topoisomerase IIα catalytic inhibitor with much stronger activity and less DNA toxicity than etoposide, a topoisomerase II poison. TI-1-190 displays caspase 3-independent anticancer activity, unlike etoposide.
ISSN:1359-7345
1364-548X
DOI:10.1039/c7cc02372c