Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone

Bioorganic & Medicinal Chemistry Letters
2008.0

Abstract

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.

Knowledge Graph

Similar Paper

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone
Bioorganic & Medicinal Chemistry Letters 2008.0
Dihydroxyphenylisoindoline Amides as Orally Bioavailable Inhibitors of the Heat Shock Protein 90 (Hsp90) Molecular Chaperone
Journal of Medicinal Chemistry 2010.0
Novel, Potent Small-Molecule Inhibitors of the Molecular Chaperone Hsp90 Discovered through Structure-Based Design
Journal of Medicinal Chemistry 2005.0
Adenine derived inhibitors of the molecular chaperone HSP90—SAR explained through multiple X-ray structures
Bioorganic & Medicinal Chemistry Letters 2004.0
Targeting the entry region of Hsp90's ATP binding pocket with a novel 6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl amide
European Journal of Medicinal Chemistry 2016.0
Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90
Journal of Medicinal Chemistry 2016.0
Combining Hit Identification Strategies: Fragment-Based and in Silico Approaches to Orally Active 2-Aminothieno[2,3-d]pyrimidine Inhibitors of the Hsp90 Molecular Chaperone
Journal of Medicinal Chemistry 2009.0
Discovery of Benzisoxazoles as Potent Inhibitors of Chaperone Heat Shock Protein 90
Journal of Medicinal Chemistry 2008.0
5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone
Bioorganic & Medicinal Chemistry Letters 2009.0
Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3- d ]pyrimidines as potent Hsp90 inhibitors
Bioorganic & Medicinal Chemistry Letters 2017.0