Design, synthesis and antitumor activity evaluation of benzimidazole derivatives with potent HDAC inhibitory activity

IF 2.6 4区医学 Q3 CHEMISTRY, MEDICINAL

Medicinal Chemistry Research Pub Date : 2024-11-21 DOI:10.1007/s00044-024-03349-2

Jiantao Ping, Hongrui Chu, Yisheng Zhao, Chen Chen

引用次数: 0

Abstract

This study aims to design and synthesize novel benzimidazole histone deacetylase (HDAC) inhibitors to explore their potential applications in the treatment of cancer and other related diseases. By comparing the structures of our reported benzimidazole HDAC inhibitors, we designed a series of compounds accordingly. We then used experimentally verified their inhibitory activity against HDAC enzymes. The results showed that several of the newly synthesized compounds showed good HDAC inhibition and anti-proliferative activity. Therefore, we conclude that these novel HDAC inhibitors have potential as drug candidates for the treatment of cancer.

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具有强HDAC抑制活性的苯并咪唑衍生物的设计、合成及抗肿瘤活性评价

本研究旨在设计合成新型苯并咪唑类组蛋白去乙酰化酶（HDAC）抑制剂，探索其在癌症等相关疾病治疗中的应用潜力。通过比较我们所报道的苯并咪唑类HDAC抑制剂的结构，我们相应地设计了一系列化合物。然后用实验验证了它们对HDAC酶的抑制活性。结果表明，新合成的几种化合物具有良好的抑制HDAC和抗增殖活性。因此，我们得出结论，这些新的HDAC抑制剂有潜力作为治疗癌症的候选药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Medicinal Chemistry Research 医学-医药化学

CiteScore

4.70

自引率

3.80%

发文量

162

审稿时长

5.0 months

期刊介绍： Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.