Author/Authors :
Colletti، نويسنده , , Steven L and Myers، نويسنده , , Robert W and Darkin-Rattray، نويسنده , , Sandra J and Schmatz، نويسنده , , Dennis M and Fisher، نويسنده , , Michael H and Wyvratt، نويسنده , , Matthew J and Meinke، نويسنده , , Peter T، نويسنده ,
Abstract :
A four step degradation of the C8 ethyl ketone of apicidin provided a route to the C6 aldehyde intermediate and several mechanism-based transition state inhibitors of histone deacetylase. The compounds generated herein delineate the significance of apicidinʹs side chain, highlighted by the high affinity C8 aldehyde and C8-keto-9,10-epoxide analogs of apicidin.
Keywords :
apicidin , Side chain , transition state inhibitors , Histone deacetylase