含 1,3,4-恶二唑的组蛋白去乙酰化酶抑制剂：在癌细胞中的抗癌活性。
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
机构信息
Department of Drug Chemistry and Technologies, Sapienza University of Rome , P. le A. Moro 5, 00185 Rome Italy.
出版信息
J Med Chem. 2014 Jul 24;57(14):6259-65. doi: 10.1021/jm500303u. Epub 2014 Jul 8.
We describe 1,3,4-oxadiazole-containing hydroxamates (2) and 2-aminoanilides (3) as histone deacetylase inhibitors. Among them, 2t, 2x, and 3i were the most potent and selective against HDAC1. In U937 leukemia cells, 2t was more potent than SAHA in inducing apoptosis, and 3i displayed cell differentiation with a potency similar to MS-275. In several acute myeloid leukemia (AML) cell lines, as well as in U937 cells in combination with doxorubicin, 3i showed higher antiproliferative effects than SAHA.
我们将含有 1,3,4-恶二唑的羟肟酸酯（2）和 2-氨基苯甲酰胺（3）描述为组蛋白去乙酰化酶抑制剂。其中，2t、2x 和 3i 对 HDAC1 的抑制作用最强且选择性最高。在 U937 白血病细胞中，2t 在诱导细胞凋亡方面比 SAHA 更有效，3i 表现出与 MS-275 相当的细胞分化作用。在几种急性髓系白血病（AML）细胞系以及与多柔比星联合使用的 U937 细胞中，3i 的抗增殖作用均高于 SAHA。
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