Details

Autor(en) / Beteiligte

• Jeon, K. H
• Park, C
• Kadayat, T. M
• Shrestha, A
• Lee, E. S
• Kwon, Y

Titel

A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activityElectronic supplementary information (ESI) available: Systematic evaluation flow, synthesis methodology and characterization, DNA binding, topo I/topo IIα-mediated supercoiled DNA relaxation, kDNA decatenation and cleavable complex assay, comet assay, H2AX phosphorylation, topo IIα-catalysed ATP hydrolysis, cytotoxicity, western blotting, and f

Erscheinungsjahr

2017-06

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5 H -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. A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5 H -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.