Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases
Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases
复制标题
作为 Cdc25 磷酸酶抑制剂的米替隆类似物的合成
DOI：
10.1016/j.bmcl.2005.12.080
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发表时间：
2006-04-01
影响因子：
2.7
通讯作者：
Lu, W
中科院分区：
文献类型：
--
作者：
Huang, WG;Li, JY;Lu, W
合成了米替隆类似物，并评价了其对Cdc 25和PTP 1B的抑制活性。大多数化合物表现出有效的Cdc 25抑制活性，和几个表现出更高的选择性Cdc 25比PTP 1B。在细胞毒性试验中，大多数化合物显示出对肿瘤细胞系A549和HCT-116的细胞毒性，产生的IC 50值在微摩尔范围内。(C)2006爱思唯尔有限公司保留所有权利。
Miltirone analogues were synthesized and evaluated for inhibitory activity against Cdc25 and PTP1B. Most of the compounds demonstrated potent Cdc25 inhibitory activity, and several exhibited higher selectivity for Cdc25 than for PTP1B. In a cytotoxic assay, most of the compounds displayed cytotoxicity against the tumor cell lines A549 and HCT-116, producing IC50 values in the micromolar range. (C) 2006 Elsevier Ltd. All rights reserved.