Discovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin.
Discovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin.
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通过调节 Dykerin 的表达发现新的 chromen-4-one 衍生物作为端粒酶抑制剂
DOI：
10.1080/14756366.2018.1466881
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发表时间：
2018-12
影响因子：
5.6
通讯作者：
Hua Liu X
中科院分区：
文献类型：
--
作者：
Quan Wang J;Di Yang M;Chen X;Wang Y;Zeng Chen L;Cheng X;Hua Liu X
摘要 设计并合成了一系列新型三甲氧基苯基-4H-苯并吡喃衍生物，通过调节dykerin作为端粒酶抑制剂。体外抗癌活性测定表明，化合物5i 3-(4-(4-isonicotinoylpiperazin-1-yl)butoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyryl)-4H-chromen-4-one对Hela、SMMC-7721、SGC-7901、U87和HepG2细胞系表现出较高的活性。化合物 5i 还显示出有效的端粒酶抑制活性。进一步的结果证实该标题化合物能够显着改善体内诱导的大鼠肝肿瘤的病理变化。初步机制表明，化合物 5i 通过降低 Dykerin 的表达来抑制端粒酶活性。
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.
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