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多靶点抗癌药物:合理方法、合成途径和构效关系。

Multi-Targeting Anticancer Agents: Rational Approaches, Synthetic Routes and Structure Activity Relationship.

机构信息

Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab-143005, India.

Program in Chemical Biology, Sloan Kettering Institute, New York, NY 10065, United States.

出版信息

Anticancer Agents Med Chem. 2019;19(7):842-874. doi: 10.2174/1871520619666190118120708.

Abstract

We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. The simultaneous interruption of two or more targets has improved the therapeutic efficacy as compared to the specific targeted based therapy. In this review, six types of dual targeting agents along with some interesting strategies used for their design and synthesis are discussed. Their pharmacology with various types of the molecular interactions within their specific targets has also been described. This assemblage will reveal the recent trends and insights in front of the scientific community working in dual inhibitors and help them in designing the next generation of multi-targeted anti-cancer agents.

摘要

我们生活在一个充满复杂疾病的世界中,如癌症,这种疾病不能用单一化合物、单一靶点的治疗模式来治愈。这可能是由于涉及多种发病机制。一化合物多靶点策略已成为抗癌药物发现的热门研究课题。与特定的靶向治疗相比,同时阻断两个或多个靶点可以提高治疗效果。在这篇综述中,讨论了六种类型的双重靶向剂以及用于其设计和合成的一些有趣策略。还描述了它们在特定靶标内各种类型分子相互作用下的药理学。这组文章将揭示在从事双重抑制剂研究的科学界面前的最新趋势和见解,并帮助他们设计下一代多靶点抗癌药物。

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