水飞蓟宾的鉴定和初步 SAR 研究：一种 HSP90 抑制剂。
Identification and initial SAR of silybin: an Hsp90 inhibitor.
机构信息
Department of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, USA.
出版信息
Bioorg Med Chem Lett. 2011 May 1;21(9):2659-64. doi: 10.1016/j.bmcl.2010.12.088. Epub 2010 Dec 28.
Through Hsp90-dependent firefly luciferase refolding and Hsp90-dependent heme-regulated eIF2α kinase (HRI) activation assays, silybin was identified as a novel Hsp90 inhibitor. Subsequently, a library of silybin analogues was designed, synthesized and evaluated. Initial SAR studies identified the essential, non-essential and detrimental functionalities on silybin that contribute to Hsp90 inhibition.
通过依赖 Hsp90 的萤火虫荧光素酶复性和依赖 Hsp90 的血红素调节的 eIF2α 激酶 (HRI) 激活测定，水飞蓟宾被鉴定为一种新型的 Hsp90 抑制剂。随后，设计、合成并评估了一系列水飞蓟宾类似物文库。初步 SAR 研究确定了水飞蓟宾中对 Hsp90 抑制有贡献的必需、非必需和有害功能。
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