Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 권영주 | * |
dc.date.accessioned | 2021-08-12T16:31:31Z | - |
dc.date.available | 2021-08-12T16:31:31Z | - |
dc.date.issued | 2021 | * |
dc.identifier.issn | 0045-2068 | * |
dc.identifier.other | OAK-29523 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/258679 | - |
dc.description.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. | * |
dc.language | English | * |
dc.publisher | Academic Press Inc. | * |
dc.subject | Anti-proliferative activity | * |
dc.subject | Benzofuro[3,2-b]pyridin-7-ol | * |
dc.subject | Halogen moiety | * |
dc.subject | Hydroxyl moiety | * |
dc.subject | Structure-activity relationship | * |
dc.subject | Topoisomerase inhibition | * |
dc.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 | * |
dc.type | Article | * |
dc.relation.volume | 111 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.journaltitle | Bioorganic Chemistry | * |
dc.identifier.doi | 10.1016/j.bioorg.2021.104884 | * |
dc.identifier.wosid | WOS:000656967400004 | * |
dc.identifier.scopusid | 2-s2.0-85104152567 | * |
dc.author.google | Thapa Magar T.B. | * |
dc.author.google | Hee Seo S. | * |
dc.author.google | Shrestha A. | * |
dc.author.google | Kim J.-A. | * |
dc.author.google | Kunwar S. | * |
dc.author.google | Bist G. | * |
dc.author.google | Kwon Y. | * |
dc.author.google | Lee E.-S. | * |
dc.contributor.scopusid | 권영주(12446435600) | * |
dc.date.modifydate | 20240422124907 | * |