Fused and Substituted Piperazines as Anticancer Agents: A Review

IF 3.3 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemical Biology & Drug Design Pub Date : 2025-03-06 DOI:10.1111/cbdd.70077
Saumya Singh, Rajnish Kumar, Shrishti Tripathi,  Salahuddin, Avijit Mazumder, Nardev Singh
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Abstract

Cancer is an abnormal and uncontrolled proliferation of normal cells. The availability of safer anticancer drugs with exceptional selectivity for healthy cells and great efficacy against various cancer forms continues to be a significant obstacle. The piperazine moiety is used as the building block of several molecules and is reported to have the ability to inhibit the cell cycle (G1/S phase), inhibit angiogenesis, and interact with DNA. Piperazine also has a flexible binding feature that allows it to interact with a variety of biological targets, which makes it effective against cancers. As there is a continuous need to obtain an anticancer drug with improved efficacy and fewer side effects, the piperazine derivatives attract the attention of researchers. This review highlights the recently reported methods of synthesis of fused/substituted piperazines, structure–activity relationship, and interactions with targets/receptors as anticancer agents. Thus, the presented review will help medicinal chemists in designing anticancer molecules with piperazines.

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融合和取代哌嗪作为抗癌药物的研究进展
癌症是正常细胞的不正常和不受控制的增殖。对健康细胞具有特殊选择性和对各种癌症形式具有巨大功效的更安全的抗癌药物的可用性仍然是一个重大障碍。哌嗪部分被用作几个分子的构建块,据报道具有抑制细胞周期(G1/S期)、抑制血管生成和与DNA相互作用的能力。哌嗪还具有灵活的结合特性,使其能够与各种生物靶标相互作用,从而有效地对抗癌症。由于人们不断需要获得一种疗效更高、副作用更小的抗癌药物,哌嗪类衍生物引起了研究人员的关注。本文综述了近年来报道的融合/取代哌嗪的合成方法、结构-活性关系以及与靶点/受体的相互作用作为抗癌药物。因此,本文的综述将有助于药物化学家设计含哌嗪的抗癌分子。
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来源期刊
Chemical Biology & Drug Design
Chemical Biology & Drug Design 医学-生化与分子生物学
CiteScore
5.10
自引率
3.30%
发文量
164
审稿时长
4.4 months
期刊介绍: Chemical Biology & Drug Design is a peer-reviewed scientific journal that is dedicated to the advancement of innovative science, technology and medicine with a focus on the multidisciplinary fields of chemical biology and drug design. It is the aim of Chemical Biology & Drug Design to capture significant research and drug discovery that highlights new concepts, insight and new findings within the scope of chemical biology and drug design.
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