206537-23-7Relevant articles and documents
COMPOUNDS AND METHODS FOR INHIBITING THE INTERACTION OF BCL PROTEINS WITH BINDING PARTNERS
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Page/Page column 67, (2008/06/13)
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Synthesis and preliminary evaluation of a library of polycyclic small molecules for use in chemical genetic assays
Tan, Derek S.,Foley, Michael A.,Stockwell, Brent R.,Shair, Matthew D.,Schreiber, Stuart L.
, p. 9073 - 9087 (2007/10/03)
(-)-Shikimic acid, 3, was converted into both enantiomers of epoxycyclohexenol carboxylic acid, 7, which were attached to a solid support via a photocleavable linker. Tandem acylation-1,3-dipolar cycloaddition with nitrones 11a-g yielded tetracyclic templates 12a-g. After development of several efficient coupling reactions of iodobenzyl tetracycles 12b-d and completion of extensive validation protocols, a splitpool synthesis yielded a binary encoded library calculated to contain 2.18 million polycyclic compounds. These compounds are compatible with miniaturized cell-based 'forward' chemical genetic assays designed to explore biological pathways and 'reverse' chemical genetic assays designed to explore protein function. As a simple illustration of the potential of these compounds, several were shown to activate a TGF-β-responsive reporter gene in mammalian cells.