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Design and synthesis of histone deacetylase inhibitors: the development of apicidin transition state analogs

✍ Scribed by Steven L Colletti; Robert W Myers; Sandra J Darkin-Rattray; Dennis M Schmatz; Michael H Fisher; Matthew J Wyvratt; Peter T Meinke

Publisher
Elsevier Science
Year
2000
Tongue
French
Weight
104 KB
Volume
41
Category
Article
ISSN
0040-4039

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✦ Synopsis

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 apicidin's side chain, highlighted by the high affinity C8 aldehyde and C8-keto-9,10-epoxide analogs of apicidin.

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