基于芳基亚磺酰基-2,4-己二烯酸羟酰胺的组蛋白去乙酰化酶芳香族硫化物抑制剂。
Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
作者信息
Marson Charles M, Savy Pascal, Rioja Alphonso S, Mahadevan Thevaki, Mikol Catherine, Veerupillai Arthi, Nsubuga Eva, Chahwan Angela, Joel Simon P
机构信息
Department of Chemistry, University College London, Christopher Ingold Laboratories, London WC1H OAJ, UK.
出版信息
J Med Chem. 2006 Jan 26;49(2):800-5. doi: 10.1021/jm051010j.
The synthesis of a novel series of potent inhibitors of histone deacetylases is described, based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides and their derivatives. In vitro IC(50) values down to 40 nM were obtained, and several compounds showed inhibition of CEM (human leukemic) cell viability with IC(50) of approximately 1.5 microM, comparable to or better than that of suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase currently in clinical trials.
本文描述了基于芳基亚磺酰基-2,4-己二烯酸羟酰胺及其衍生物的一系列新型高效组蛋白脱乙酰酶抑制剂的合成。体外IC(50)值低至40 nM，几种化合物对CEM（人白血病）细胞活力的抑制作用的IC(50)约为1.5 microM，与目前正在进行临床试验的组蛋白脱乙酰酶抑制剂辛二酰苯胺异羟肟酸相当或更好。
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