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首页> 外文期刊>Drug Design, Development and Therapy >Novel HDAC/Tubulin Dual Inhibitor: Design, Synthesis and Docking Studies of α-Phthalimido-Chalcone Hybrids as Potential Anticancer Agents with Apoptosis-Inducing Activity
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Novel HDAC/Tubulin Dual Inhibitor: Design, Synthesis and Docking Studies of α-Phthalimido-Chalcone Hybrids as Potential Anticancer Agents with Apoptosis-Inducing Activity

机译：新型HDAC /管蛋白双抑制剂：α-酞胺 - 丙酮杂交物的设计，合成和对接研究作为具有凋亡诱导活性的潜在抗癌剂

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Introduction: In order to develop novel anticancer HDAC/tubulin dual inhibitors, a novel series of α-phthalimido-substituted chalcones-based hybrids was synthesized and characterized by IR, 1H NMR, 13C NMR, mass spectroscopy and X-ray analysis. Methods: All the synthesized compounds were evaluated for their in vitro anticancer activity against MCF-7 and HepG2 human cancer cell lines using MTT assay. To explore the mechanism of action of the synthesized compounds, in vitro β -tubulin polymerization and HDAC 1 and 2 inhibitory activity were measured for the most potent anticancer hybrids. Further, cell cycle analysis was also evaluated. Results: The trimethoxy derivative 7j showed the most potent anticancer activity, possessed the most potent β -tubulin polymerase and HDAC 1 and 2 inhibitory activity and efficiently induced cell cycle arrest at both G2/M and preG1phases in the MCF-7 cell line.
机译：介绍：为了开发新的抗癌HDAC /管蛋白双抑制剂，通过IR，1H NMR，13C NMR，质谱和X射线分析合成了一种基于α-酞米胺取代的基氨基酮的杂交杂交物。方法：使用MTT测定评价所有合成的化合物对MCF-7和HepG2人癌细胞系的体外抗癌活性。为了探讨合成化合物的作用机制，测量体外β-丁蛋白聚合和HDAC 1和2抑制活性的最有效的抗癌杂交。此外，还评估细胞循环分析。结果：三氧基氧化衍生物7J显示出最有效的抗癌活性，具有最有效的β-丁香蛋白聚合酶和HDAC 1和2抑制活性，并有效地在MCF-7细胞系中的G2 / M和PREG1PHASE中诱导细胞周期停滞。

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