- Discovery of novel aminoquinazolin-7-yl 6,7-dihydro-indol-4-ones as potent, selective inhibitors of heat shock protein 90
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A novel class of Hsp90 inhibitors, structurally distinct from previously reported scaffolds, was developed from rational design and optimization of a compound library screen hit. These aminoquinazoline derivatives, represented by compound 15 (SNX-6833) or 1-(2-amino-4-methylquinazolin-7-yl)-3,6,6-trimethyl-6, 7-dihydro-1H-indol-4(5H)-one, selectively bind to Hsp90 and inhibit its cellular activities at concentrations as low as single digit nanomolar.
- Huang, Kenneth H.,Barta, Thomas E.,Rice, John W.,Smith, Emilie D.,Ommen, Andy J.,Ma, Wei,Veal, James M.,Fadden, R. Patrick,Barabasz, Amy F.,Foley, Briana E.,Hughes, Philip F.,Hanson, Gunnar J.,Markworth, Christopher J.,Silinski, Melanie,Partridge, Jeffrey M.,Steed, Paul M.,Hall, Steven E.
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scheme or table
p. 2550 - 2554
(2012/05/20)
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- Isoquinoline, Quinazoline and Phthalazine Derivatives
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Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R0, R5, R6, R7, n, Q1-Q5, Y, and X1-X3 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
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Page/Page column 45
(2008/06/13)
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