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

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...

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Bibliographic Details
Published in:Journal of enzyme inhibition and medicinal chemistry 2018-01, Vol.33 (1), p.1199-1211
Main Authors: Quan Wang, Jie, Di Yang, Meng, Chen, Xing, Wang, Yang, Zeng Chen, Liu, Cheng, Xiu, Hua Liu, Xin
Format: Article
Language:English
Subjects:
anticancer activity
chromen
dyskerin
Short Communication
Synthesis
telomerase activity
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Summary: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.
ISSN:1475-6366
1475-6374
DOI:10.1080/14756366.2018.1466881