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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase.
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Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase.

机译：异噻唑酮和1-异噻唑酮氧化物的反应性可抑制PCAF组蛋白乙酰转移酶。

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摘要

Development of small molecule inhibitors of the histone acetyltransferase p300/CBP associated factor (PCAF) is relevant for oncology. The inhibition of the enzyme PCAF and proliferation of the cancer cell line HEP G2 by a series of 5-chloroisothiazolones was compared to a series of 5-chloroisothiazolone-1-oxides. The PCAF inhibitory potency of 5-chloroisothiazolones and 5-chloroisothiazolone-1-oxides is influenced by substitution in the 4-position. A study on the reactivity of the HAT inhibitors towards thiols and thiolates indicates that 5-chloroisothiazolones reacted quickly with propane-1-thiolate to provide many products, whereas 5-chloroisothiazolone-1-oxides provide only one defined product. Growth inhibition studies indicate that 5-chloroisothiazolones inhibit proliferation of HEP G2 cells at concentrations between 8.6 and 24 microM, whereas 5-chloroisothiazolone-1-oxides required higher concentrations or showed no inhibition.
机译：组蛋白乙酰转移酶p300 / CBP相关因子（PCAF）小分子抑制剂的开发与肿瘤学有关。将一系列5-氯异噻唑酮对氧化酶PCAF的抑制和癌细胞系HEP G2的增殖与一系列5-氯异噻唑酮-1-氧化物进行比较。 5-氯异噻唑酮和5-氯异噻唑酮-1-氧化物的PCAF抑制能力受4-位取代的影响。对HAT抑制剂对硫醇和硫醇盐的反应性的研究表明，5-氯异噻唑酮与1-硫代丙烷反应很快，从而提供了许多产物，而5-氯异噻唑酮-1-氧化物仅提供了一种确定的产物。生长抑制研究表明，5-氯异噻唑酮在8.6和24 microM之间抑制HEP G2细胞的增殖，而5-氯异噻唑酮-1-氧化物需要更高的浓度或没有抑制作用。

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