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Synthesis and SAR study of new hydroxy and chloro-substituted 2,4-diphenyl 5H-chromeno[4,3-b]pyridines as selective topoisomerase IIα-targeting anticancer agents

Title
Synthesis and SAR study of new hydroxy and chloro-substituted 2,4-diphenyl 5H-chromeno[4,3-b]pyridines as selective topoisomerase IIα-targeting anticancer agents
Authors
Magar T.B.T.Seo S.H.Kadayat T.M.Jo H.Shrestha A.Bist G.Katila P.Kwon Y.Lee E.-S.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2018
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
Bioorganic and Medicinal Chemistry vol. 26, no. 8, pp. 1909 - 1919
Keywords
5H-Chromeno[4,3-b]pyridinesAnticancer agentsHydroxyl and chlorine-substitutionSAR studySelective topoisomerase IIα inhibition
Publisher
Elsevier Ltd
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
As part of our effort to develop potential topoisomerase IIα (topo IIα) targeting anticancer agents, we systematically designed a new series of hydroxy and chloro-substituted 2,4-diphenyl 5H-chromeno[4,3-b]pyridines. Total eighteen compounds were synthesized and tested for their ability to inhibit the function of topo I and IIα and proliferation of human breast (T47D), colorectal (HCT15), and cervix (HeLa) cancer cells. Except compound 11, all of the tested compounds displayed selective topo IIα inhibitory activity. Compounds 8–18, 22, 24, and 25 showed excellent topo IIα inhibitory activity than a positive control, etoposide. Most of the compounds appeared to be superior to reference compounds in their antiproliferative activity. Structure-activity relationship (SAR) study has shown that it is better to place the hydroxyphenyl group at the 4-position of the central pyridine for superior topo IIα inhibition and antiproliferative activity. Similarly, the 3′-, or 4′-hydroxyphenyl substitution at the 2- and 4-positon of pyridine ring is important for better activity than 2′-substitution. © 2018 Elsevier Ltd
DOI
10.1016/j.bmc.2018.02.035
Appears in Collections:
약학대학 > 약학과 > Journal papers
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