Inventors:
Gabriela Chiosis - New York NY, US
Huazhong He - New York NY, US
Joungnam Kim - Forest Hills NY, US
Steven M. Larson - New York NY, US
Peter Smith-Jones - New York NY, US
Assignee:
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH - New York NY
International Classification:
A61K 31/52, C07D 473/34, A61P 35/00, A61K 51/00, A61P 43/00, C12N 5/02
US Classification:
424 165, 544276, 544277, 51426324, 51426337, 5142634, 435375
Abstract:
Hsp90 inhibitors having are provided having the formula:with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SOalkyl, COO-alkyl, KH, OH, CN, SOX, NO, NO, C═SRNSOX, C═OR, where Xis F, NH2, alkyl or H, and Ris alkyl, NH, NH-alkyl or O-alkyl, Cto Calkyl or alkoxy; or wherein Xhas the formula -0-(CH)-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.