Abstract
A chimera composed of the natural products radicicol and geldanamycin has been prepared through an amide linkage connecting the resorcinol moiety of radicicol to the quinone ring of geldanamycin. The inhibitory activity of these compounds was determined by their ability to inhibit Hsp90's inherent ATPase activity along with degradation of the Hsp90 client protein, HER-2 in MCF-7 breast cancer cells. [reaction: see text]
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Acetanilides / chemistry
-
Acetanilides / pharmacology*
-
Adenosine Triphosphatases / antagonists & inhibitors
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / pharmacology
-
Benzoates / chemistry
-
Benzoates / pharmacology*
-
Benzoquinones
-
Breast Neoplasms / drug therapy*
-
Breast Neoplasms / pathology
-
Cell Line, Tumor
-
Drug Design
-
Female
-
HSP90 Heat-Shock Proteins / antagonists & inhibitors
-
Humans
-
Lactams, Macrocyclic
-
Lactones / chemistry
-
Lactones / pharmacology*
-
Macrolides
-
Quinones / chemistry
-
Quinones / pharmacology*
-
Receptor, ErbB-2 / antagonists & inhibitors
-
Receptor, ErbB-2 / metabolism
Substances
-
Acetanilides
-
Antineoplastic Agents
-
Benzoates
-
Benzoquinones
-
HSP90 Heat-Shock Proteins
-
Lactams, Macrocyclic
-
Lactones
-
Macrolides
-
Quinones
-
radamide
-
Receptor, ErbB-2
-
Adenosine Triphosphatases
-
monorden
-
geldanamycin