Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.
Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.
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DOI：
10.1016/j.bmcl.2006.12.117
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发表时间：
2007-03
影响因子：
2.7
通讯作者：
Takayoshi Suzuki;Shinya Hisakawa;Yukihiro Itoh;S. Maruyama;Mineko Kurotaki;H. Nakagawa;N. Miyata
中科院分区：
文献类型：
--
作者：
Takayoshi Suzuki;Shinya Hisakawa;Yukihiro Itoh;S. Maruyama;Mineko Kurotaki;H. Nakagawa;N. Miyata
为了鉴定硫醇盐组蛋白脱乙酰酶抑制剂NCH-31的前药，其显示出有效的抗增殖活性并且在人血浆中稳定，我们合成了NCH-31的几种候选前药。在这些化合物中，S-2-甲基-3-苯丙酰基化合物2显示出比S-异丁酰基化合物NCH-51更有效的抗增殖活性和在人血浆中更高的稳定性。
To identify prodrugs of a thiolate histone deacetylase inhibitor NCH-31 that show potent antiproliferative activity and are stable in human plasma, we synthesized several candidate prodrugs of NCH-31. Among these compounds, S-2-methyl-3-phenylpropanoyl compound 2 showed more potent antiproliferative activity and higher stability in human plasma than S-isobutyryl compound NCH-51.