Discovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin

Autor:	Jie Quan Wang, Meng Di Yang, Xing Chen, Yang Wang, Liu Zeng Chen, Xiu Cheng, Xin Hua Liu
Jazyk:	angličtina
Rok vydání:	2018
Předmět:	Synthesis chromen anticancer activity dyskerin telomerase activity Therapeutics. Pharmacology RM1-950
Zdroj:	Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 33, Iss 1, Pp 1199-1211 (2018)
Druh dokumentu:	article
ISSN:	1475-6366 1475-6374 14756366
DOI:	10.1080/14756366.2018.1466881
Popis:	A series of new trimethoxyphenyl-4H-chromen derivatives as telomerase inhibitors through regulation dyskerin were designed and synthesised. The anticancer activity assay in vitro showed that compound 5i 3-(4-(4-isonicotinoylpiperazin-1-yl)butoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one exhibited high activity against Hela, SMMC-7721, SGC-7901, U87 and HepG2 cell lines. Compound 5i also showed potent inhibitory activity against telomerase. The further results confirmed this title compound could significantly improve pathological changes induced rat hepatic tumor in vivo. Preliminary mechanisms showed that compound 5i inhibited telomerase activity through decrease expression of dyskerin.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/38353f8152524ba291bbb1e51445926e Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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