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

ABSTRACT: 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.

SUBMITTER: Quan Wang J

PROVIDER: S-EPMC6104605 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

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

Quan Wang Jie J Di Yang Meng M Chen Xing X Wang Yang Y Zeng Chen Liu L Cheng Xiu X Hua Liu Xin X

Journal of enzyme inhibition and medicinal chemistry 20181201 1

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 titl ...[more]

PMID: 30132373

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