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A new phenolic series of indenopyridinone as topoisomerase inhibitors: Design, synthesis, and structure-activity relationships

Title
A new phenolic series of indenopyridinone as topoisomerase inhibitors: Design, synthesis, and structure-activity relationships
Authors
Shrestha, AarajanaPark, SeojeongJang, Hae JinKatila, PramilaShrestha, RitinaKwon, YoungjooLee, Eung-Seok
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2018
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN
0968-0896JCR Link

1464-3391JCR Link
Citation
BIOORGANIC & MEDICINAL CHEMISTRY vol. 26, no. 18, pp. 5212 - 5223
Keywords
IndenopyridinonePhenolic groupTopoisomerase inhibitorDNA intercalatorAnti-proliferative activity
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
DNA Topoisomerase II alpha (topo II alpha) is one of the most effective therapeutic targets to control cancer. In an effort to develop novel and effective topo II alpha targeting anti-proliferative agent, a phenolic series of indenopyridinone and indenopyridinol were designed and prepared using efficient multi-component one pot synthetic method. Total twenty-two synthesized compounds were assessed for topo I and II alpha inhibition, and anti-proliferation in three different human cancer cell lines. Overall structure-activity relationship study explored the significance of meta-phenolic group at 4-position and para-phenolic group at 2- and/or 4-position of indenopyridinone skeleton for strong topo II alpha-selective inhibition and anti-proliferative activity against human cervix (HeLa) and colorectal (HCT15) cell lines. Compound 12 with excellent topo II alpha inhibition (93.7%) was confirmed as a DNA intercalator that could be a new promising lead to develop effective topo II alpha-targeted anticancer agents.
DOI
10.1016/j.bmc.2018.09.021
Appears in Collections:
약학대학 > 약학과 > Journal papers
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