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; Y. Kwon

doi:10.1039/c7cc02372c

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, Y. Kwon

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

18 Scopus citations

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.

Original language	English
Pages (from-to)	6864-6867
Number of pages	4
Journal	Chemical Communications
Volume	53
Issue number	51
DOIs	https://doi.org/10.1039/c7cc02372c
State	Published - 2017

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© 2017 The Royal Society of Chemistry.

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

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.",

author = "Jeon, {K. H.} and C. Park and Kadayat, {T. M.} and A. Shrestha and Lee, {E. S.} and Y. Kwon",

note = "Publisher Copyright: {\textcopyright} 2017 The Royal Society of Chemistry.",

year = "2017",

doi = "10.1039/c7cc02372c",

language = "English",

volume = "53",

pages = "6864--6867",

journal = "Chemical Communications",

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publisher = "Royal Society of Chemistry",

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T1 - A novel indeno[1,2-b] pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity

AU - Jeon, K. H.

AU - Park, C.

AU - Kadayat, T. M.

AU - Shrestha, A.

AU - Lee, E. S.

AU - Kwon, Y.

PY - 2017

Y1 - 2017

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=85021767786&partnerID=8YFLogxK

U2 - 10.1039/c7cc02372c

DO - 10.1039/c7cc02372c

M3 - Article

C2 - 28604852

AN - SCOPUS:85021767786

SN - 1359-7345

VL - 53

SP - 6864

EP - 6867

JO - Chemical Communications

JF - Chemical Communications

IS - 51

ER -

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

Abstract

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