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Isoform-selective HDAC1/6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity

A series of hydroxamic acids linked by different lengths to a chiral imidazo-ketopiperazine scaffold were synthesized. The compounds with linker lengths of 6 and 7 carbon atoms were the most potent in histone deacetylase (HDAC) inhibition, and were specific submicromolar inhibitors of the HDAC1, HDA...

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Veröffentlicht in:Philos Trans R Soc Lond B Biol Sci
Hauptverfasser: Lecointre, Bertrand, Narozny, Remy, Borrello, Maria Teresa, Senger, Johanna, Chakrabarti, Alokta, Jung, Manfred, Marek, Martin, Romier, Christophe, Melesina, Jelena, Sippl, Wolfgang, Bischoff, Laurent, Ganesan, A.
Format: Artigo
Sprache:Inglês
Veröffentlicht: The Royal Society 2018
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Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5915728/
https://ncbi.nlm.nih.gov/pubmed/29685969
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1098/rstb.2017.0364
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