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N-甲基吡啶酰胺在抗癌治疗药物开发中的意义:合成与构效关系(SAR)研究。

The significance of N-methylpicolinamides in the development of anticancer therapeutics: Synthesis and structure-activity relationship (SAR) studies.

机构信息

Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan 430070, PR China.

Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan 430070, PR China.

出版信息

Bioorg Chem. 2019 May;86:513-537. doi: 10.1016/j.bioorg.2019.02.030. Epub 2019 Feb 13.

DOI:10.1016/j.bioorg.2019.02.030
PMID:30782571
Abstract

Cancer is the second most important cause of death worldwide. There is always a demand for new anticancer drugs and continuously a wide variety of natural and synthetic compounds were developed by the researchers. Nowadays, a large number of drugs in clinical practice were found to have a high incidence of side effect and multidrug conflict. The development of novel less toxic, low cost and very energetic N-methylpicolinamide-bearing hybrids is a hot research topic in the community of medicinal chemistry. Herein we highlight the current advances in the synthesis of picolinamide-containing heterocyclic compounds as potent anticancer agents. In addition, briefly explore their structure-activity relationship studies for the inspiration of the innovation and development of more potent and effective drugs against various death-causing cancer diseases.

摘要

癌症是全球第二大死亡原因。人们一直对新型抗癌药物有需求,研究人员也在不断开发各种天然和合成化合物。如今,大量在临床实践中使用的药物被发现具有很高的副作用发生率和多药冲突。因此,开发新型、低毒、低成本且非常有效的含 N-甲基吡啶酰胺的杂合体是药物化学领域的热门研究课题。本文重点介绍了合成含吡啶酰胺杂环化合物作为有效抗癌药物的最新进展。此外,还简要探讨了它们的构效关系研究,为创新和开发更多针对各种致命癌症疾病的更有效药物提供了启示。

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