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Identification of new halogen-containing 2,4-diphenyl indenopyridin-5-one derivative as a boosting agent for the anticancer responses of clinically available topoisomerase inhibitors

Title
Identification of new halogen-containing 2,4-diphenyl indenopyridin-5-one derivative as a boosting agent for the anticancer responses of clinically available topoisomerase inhibitors
Authors
Hwang S.-Y.Shrestha A.Park S.Bist G.Kunwar S.Kadayat T.M.Jang H.Seo M.Sheen N.Kim S.Jeon K.-H.Lee E.-S.Kwon Y.
Ewha Authors
권영주전경화
SCOPUS Author ID
권영주scopus
Issue Date
2022
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
European Journal of Medicinal Chemistry vol. 227
Publisher
Elsevier Masson s.r.l.
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Based on previous reports on the significance of halogen moieties and the indenopyridin-5-one skeleton, we designed and synthesized a novel series of halogen (F−, Cl−, Br−, CF3− and OCF3−)-containing 2,4-diphenyl indenopyridin-5-ones and their corresponding -5-ols. Unlike indenopyridin-5-ols, most of the prepared indenopyridin-5-ones with Cl−, Br−, and CF3− groups at the 2-phenyl ring conferred a strong dual topoisomerase I/IIα inhibitory effect. Among the series, para-bromophenyl substituted compound 9 exhibited the most potent topoisomerase inhibition and antiproliferative effects, which showed dependency upon the topoisomerase gene expression level of diverse cancer cells. In particular, as a DNA minor groove-binding non-intercalative topoisomerase I/IIα catalytic inhibitor, compound 9 synergistically promoted the anticancer efficacy of clinically applied topoisomerase I/IIα poisons both in vitro and in vivo, having the great advantage of alleviating poison-related toxicities. © 2021 Elsevier Masson SAS
DOI
10.1016/j.ejmech.2021.113916
Appears in Collections:
약학대학 > 약학과 > Journal papers
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