- Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides
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The synthesis of a novel series of potent inhibitors of histone deacetylases is described, based on arylsulfinyl-2,4-hexadienoic acid hydroxyamicles and their derivatives. In vitro IC50 values clown to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC50 of ~1.5 μM, comparable to or better than that of suberoylatiilide hydroxamic acid, an inhibitor of histone cleacetylase currently in clinical trials.
- Marson, Charles M.,Savy, Pascal,Rioja, Alphonse S.,Mahadevan, Thevaki,Mikol, Catherine,Veerupillai, Arthi,Nsubuga, Eva,Chahwan, Angela,Joel, Simon P.
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p. 800 - 805
(2007/10/03)
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- HISTONE DEACETYLASE INHIBITORS
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The present invention provides histone deacetylase inhibitors of general formula (I), process for the preparation of such compounds and uses of the compounds in medicine.
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