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Bioorg Med Chem Lett
; 25(6): 1338-42, 2015 Mar 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-25677667
RESUMEN
Two novel series of oxazepine and diazepine based HSP90 inhibitors are reported. This effort relied on structure based design and isothermal calorimetry to identify small drug like macrocycles. Computational modelling was used to build into a solvent exposed pocket near the opening of the ATP binding site, which led to potent inhibitors of HSP90 (25-30).