Hydroxylated 2,4-diphenyl indenopyridine derivatives as a selective non-intercalative topoisomerase catalytic inhibitor
- 주제(키워드) Anticancer agents , catalytic inhibitorAntiproliferative activity , Hydroxylated 2 , 4-diphenyl indenopyridine , Terpyridine , Topoisomerase IIa non-intercalative
- 등재 SCIE, SCOPUS
- 발행기관 Elsevier Masson SAS
- 발행년도 2014
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000113160
- 본문언어 영어
- Published As http://dx.doi.org/10.1016/j.ejmech.2014.11.046
초록/요약
For the development of novel anticancer agents, we designed and synthesized hydroxylated 2,4-diphenyl indenopyridines, and evaluated their topoisomerase inhibitory activity as well as their antiproliferative activities against several human cancer cell lines. The structure-activity relationship study showed that indenopyridines with hydroxyl group at meta or para positions of 2-or 4-phenyl ring displayed selective and significant topoisomerase IIα (topo IIα) inhibitory activity and potent antiproliferative activity. Positive correlation between topo IIα inhibition and antiproliferative activity was observed for compounds 15, 16, 18-20, 22, 23, 25 and 26. The mode of action of compound 16 was further evaluated to be a non-intercalativetopo IIα catalytic inhibitor.
more