title: A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.
abstract: Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin. These compounds show class I subtype selectivity and levels of cellular activity comparable to clinical candidates. A representative example has demonstrated tumor growth inhibition in a human colon HCT-116 carcinoma xenograft model comparable to known inhibitors.
authors: IRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy. philip_jones@merck.com
authors: Philip
authors: P
authors: Jones
authors: Sergio
authors: S
authors: Altamura
authors: Raffaele
authors: R
authors: De Francesco
authors: Odalys Gonzalez
authors: OG
authors: Paz
authors: Olaf
authors: O
authors: Kinzel
authors: Giuseppe
authors: G
authors: Mesiti
authors: Edith
authors: E
authors: Monteagudo
authors: Giovanna
authors: G
authors: Pescatore
authors: Michael
authors: M
authors: Rowley
authors: Maria
authors: M
authors: Verdirame
authors: Christian
authors: C
authors: Steinkühler
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000737:chemistry; D006801:Humans; D007659:Ketones / Q000494:pharmacology*; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D007659:Ketones; D006655:Histone Deacetylases