Synthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuines.,ChemMedChem

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Synthesis and Anticancer Properties of Oxazepines Related to Azaisoerianin and IsoCoQuines.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-06-02 , DOI: 10.1002/cmdc.202000197
Ilhem Khelifi ₁ , Shannon Pecnard ₁ , Guillaume Bernadat ₁ , Jérome Bignon ₂ , Hélène Levaique ₂ , Joëlle Dubois ₂ , Olivier Provot ₁ , Mouad Alami ₁

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In this article, we report the synthesis and biological properties of a series of novel oxazepines related to isoCA‐4 having significant antitumor properties. Among them, three oxazepin‐9‐ol derivatives display a nanomolar or a sub‐nanomolar cytotoxicity level against five human cancer cell lines (HCT116, U87, A549, MCF7, and K562). It was demonstrated that the lead compound in this series inhibits tubulin assembly with an IC₅₀ value of 1 μM and totally arrests the cellular cycle in the G2/M phase at the low concentration of 5 nM in HCT116 and K562 cells. Molecular modeling studies perfectly corroborates these promising results.

中文翻译：

与氮杂异壬宁和IsoCoQuines相关的奥氮平的合成及其抗癌特性。

在本文中，我们报告了与具有重要抗肿瘤特性的iso CA-4相关的一系列新型奥氮平的合成和生物学特性。其中，三种oxazepin-9-ol衍生物对五种人类癌细胞系（HCT116，U87，A549，MCF7和K562）表现出纳摩尔或亚纳摩尔水平的细胞毒性水平。已证明该系列中的先导化合物以1μM的IC ₅₀值抑制微管蛋白组装，并在HCT116和K562细胞中以5 nM的低浓度完全阻止G2 / M期的细胞周期。分子建模研究完全证实了这些有希望的结果。

更新日期：2020-06-02

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