Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

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• 作者：Weigang Huang ; Jingya Li ; Wei Zhang ; Yueyang Zhou ; Chuanming Xie ; Yu Luo ; Yunfei Li ; Jingli Wang ; Jia Li and Wei Lu
• 关键词：Miltirone ; Cdc25 phosphatases ; Cancer
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 April 2006
• 年：2006
• 卷：16
• 期：7
• 页码：1905-1908
• 全文大小：100 K

文摘

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.