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Development of a purine-scaffold novel class of Hsp90 binders that inhibit the proliferation of cancer cells and induce the degradation of Her2 tyrosine kinase.

Abstract：

: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. Induces the degradation of Her2 tyrosine kinase and arrests the MCF-7 breast cancer cell line at low micromolar concentrations (IC50=2 microM).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Chiosis G,Lucas B,Shtil A,Huezo H,Rosen N

doi

10.1016/s0968-0896(02)00253-5

subject

Has Abstract

pub_date

2002-11-01 00:00:00

pages

3555-64

issue

11

eissn

0968-0896

issn

1464-3391

pii

S0968089602002535

journal_volume

10

pub_type

杂志文章

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