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一种改进的 19 取代geldanamycin 途径作为新型 HSP90 抑制剂 - 在癌症和神经退行性疾病中的潜在治疗方法。

An improved route to 19-substituted geldanamycins as novel Hsp90 inhibitors--potential therapeutics in cancer and neurodegeneration.

机构信息

School of Chemistry, University of Nottingham, University Park, Nottingham, UKNG7 2RD.

出版信息

Chem Commun (Camb). 2013 Oct 4;49(76):8441-3. doi: 10.1039/c3cc43457e.

DOI:10.1039/c3cc43457e
PMID:23770604
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3835074/
Abstract

19-Substituted geldanamycin derivatives are efficient Hsp90 inhibitors, without the toxicity associated with the other benzoquinone ansamycins, thus giving them potential for use as molecular therapeutics in cancer and neurodegeneration. Here a new method of synthesising these important compounds is reported, eliminating the need for toxic metals and metalloids.

摘要

19-取代格尔德霉素衍生物是高效的 HSP90 抑制剂，没有与其他苯醌安莎霉素相关的毒性，因此它们有可能作为癌症和神经退行性疾病的分子治疗药物。本文报道了一种新的合成这些重要化合物的方法，无需使用有毒金属和类金属。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/9b2f095e1950/c3cc43457e-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/c4975882e729/c3cc43457e-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/8f4353233a13/c3cc43457e-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/9b2f095e1950/c3cc43457e-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/c4975882e729/c3cc43457e-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/8f4353233a13/c3cc43457e-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e48/3835074/9b2f095e1950/c3cc43457e-s1.jpg

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