1.
Bioorg Med Chem Lett
; 18(23): 6273-8, 2008 Dec 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18929486
RESUMEN
Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC(50) values averaging 20 nM.