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从大自然中学习:新型格尔德霉素和雷帕霉素衍生物类 HSP90 抑制剂的研究进展

Learning from nature: advances in geldanamycin- and radicicol-based inhibitors of Hsp90.

机构信息

School of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, UK.

出版信息

J Org Chem. 2013 Jun 7;78(11):5117-41. doi: 10.1021/jo4002849. Epub 2013 Mar 26.

Abstract

Natural products have been fundamental in the development of new therapeutic agents predicated on the inhibition of heat shock protein 90 (Hsp90). This Perspective describes the influential role of the benzoquinone ansamycin geldanamycin and the resorcylic acid macrolactone radicicol not only in driving forward drug discovery programs but also in inspiring organic chemists to develop innovative methodology for the synthesis of natural products and analogues with improved properties.

摘要

天然产物在基于抑制热休克蛋白 90(Hsp90)的新型治疗药物的开发中一直起着重要作用。本观点不仅描述了苯醌类安莎霉素格尔德霉素和雷杜霉素的重要作用,推动了药物发现计划,还激发了有机化学家开发具有改进性能的天然产物和类似物的创新方法。

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