2. Academic Validation
  3. Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

  • Bioorg Med Chem Lett. 2006 Apr 1;16(7):1905-8. doi: 10.1016/j.bmcl.2005.12.080.
Weigang Huang 1,  Jingya Li,  Wei Zhang,  Yueyang Zhou,  Chuanming Xie,  Yu Luo,  Yunfei Li,  Jingli Wang,  Jia Li,  Wei Lu
Affiliations

Affiliation

  • 1 The National Center for Drugs Screening, Shanghai Institute of Materia Medica, SIBS, Graduate School of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, China.
PMID: 16434190 DOI: 10.1016/j.bmcl.2005.12.080
Abstract

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 IC(50) values in the micromolar range.

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