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Issue 51, 2017
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A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity

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Abstract

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.

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

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Publication details

The article was received on 28 Mar 2017, accepted on 29 May 2017 and first published on 31 May 2017


Article type: Communication
DOI: 10.1039/C7CC02372C
Citation: Chem. Commun., 2017,53, 6864-6867
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    A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity

    K. H. Jeon, C. Park, T. M. Kadayat, A. Shrestha, E. S. Lee and Y. Kwon, Chem. Commun., 2017, 53, 6864
    DOI: 10.1039/C7CC02372C

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