Novel Polyamine–Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming,ACS Medicinal Chemistry Letters

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Novel Polyamine–Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-11-04 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00289
Alice Pasini ₁ , Chiara Marchetti ₂ , Claudia Sissi ₃ , Marilisa Cortesi ₁ , Emanuele Giordano _{1,

4,

5} , Anna Minarini ₂ , Andrea Milelli ₆

Affiliation

A series of hybrid compounds was designed to target histone deacetylases and ds-/G-quadruplex DNAs by merging structural features deriving from Scriptaid and compound 1. Compound 6 binds different DNA arrangements, inhibits HDACs both in vitro and in cells, and is able to induce a reduction of cell proliferation. Moreover, compound 6 displays cell phenotype-reprogramming properties since it prevents the epithelial to mesenchymal transition in cancer cells, inducing a less aggressive and migratory phenotype, which is one of the goals of present innovative strategies in cancer therapies.

中文翻译：

新型多胺-萘二酰亚胺结合靶向组蛋白脱乙酰基酶和DNA用于癌症表型重编程。

通过融合源自Scriptaid和化合物1的结构特征，设计了一系列杂化化合物以靶向组蛋白脱乙酰基酶和ds- / G-四链体DNA 。化合物6结合不同的DNA排列，在体外和细胞中均抑制HDAC ，并能够诱导细胞增殖的减少。此外，化合物6显示出细胞表型的重编程特性，因为它防止了癌细胞中上皮向间质的转变，诱导了侵略性和迁移性较低的表型，这是目前癌症治疗中创新策略的目标之一。

更新日期：2017-11-04

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