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pubmed-article:16987657pubmed:abstractTextHistone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy and the first generation HDAC inhibitors are currently in clinical trials. A structurally novel series of HDAC inhibitors based on the natural cyclic tetrapeptide Apicidin is described. Selected screening of the sample collection looking for L-2-amino-8-oxodecanoic acid (L-Aoda) derivatives identified a small acyclic lead molecule 1 with the unusual ketone zinc binding group. SAR studies around this lead resulted in optimization to potent, low molecular weight, selective, non-hydroxamic acid HDAC inhibitors, equipotent to current clinical candidates.lld:pubmed
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pubmed-article:16987657pubmed:articleTitleA series of novel, potent, and selective histone deacetylase inhibitors.lld:pubmed
pubmed-article:16987657pubmed:affiliationIRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy. philip_jones@merck.com <philip_jones@merck.com>lld:pubmed
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