View : 679 Download: 0
Synthesis and structure-activity relationships of hydroxylated and halogenated 2,4-diaryl benzofuro[3,2-b]pyridin-7-ols as selective topoisomerase IIα inhibitors
- Title
- Synthesis and structure-activity relationships of hydroxylated and halogenated 2,4-diaryl benzofuro[3,2-b]pyridin-7-ols as selective topoisomerase IIα inhibitors
- Authors
- Thapa Magar T.B.; Hee Seo S.; Shrestha A.; Kim J.-A.; Kunwar S.; Bist G.; Kwon Y.; Lee E.-S.
- Ewha Authors
- 권영주
- SCOPUS Author ID
- 권영주
- Issue Date
- 2021
- Journal Title
- Bioorganic Chemistry
- ISSN
- 0045-2068
- Citation
- Bioorganic Chemistry vol. 111
- Keywords
- Anti-proliferative activity; Benzofuro[3,2-b]pyridin-7-ol; Halogen moiety; Hydroxyl moiety; Structure-activity relationship; Topoisomerase inhibition
- Publisher
- Academic Press Inc.
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- The objective of this study was to discover potential topoisomerase (topo) targeting anticancer agents. Novel series of hydroxylated and halogenated (-F, -Cl, and -CF3) 2,4-diaryl benzofuro[3,2-b]pyridin-7-ols were systematically designed and synthesized by faster, economic, and environmentally friendly l-proline catalyzed and microwave-assisted one pot reaction method. The synthesized compounds were assessed for topo I and IIα inhibitory and anti-proliferative activities. The in vitro evaluation displayed that most of the compounds have selective topo IIα inhibitory activity as well as selectivity towards T47D human cancer cell line. Structure-activity relationship study suggested that the introduction of additional hydroxyl functionality at 7-positon of benzofuro[3,2-b]pyridine skeleton is crucial for selective topo IIα inhibitory activity. Placement of phenolic moiety on the 4-position of the tricyclic system imparts better topo IIα inhibitory and anti-proliferative activity. © 2021 Elsevier Inc.
- DOI
- 10.1016/j.bioorg.2021.104884
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
- Files in This Item:
There are no files associated with this item.
- Export
- RIS (EndNote)
- XLS (Excel)
- XML