期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 10, 期 11, 页码 3555-3564出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(02)00253-5
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资金
- NCI NIH HHS [1U01 CA91178-01] Funding Source: Medline
The first published synthesis and characterization of a purine-scaffold library of hsp90 inhibitors is presented. The purine-scaffold represents a platform for the creation of easily synthesizable and derivatizable soluble molecules that are amenable for oral administration. The most active compound of the series (71) exhibits binding to hsp90 comparable to the natural product derivative 17AAG that is now in Phase I clinical trial as a cancer therapeutic. 71 Induces the degradation of Her2 tyrosine kinase and arrests the MCF-7 breast cancer cell line at low micromolar concentrations (IC50 = 2 muM). (C) 2002 Elsevier Science Ltd. All rights reserved.
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