首页> 美国政府科技报告 >New Class of Serine and Cysteine Protease Inhibitor with ChemotherapeuticPotential
【24h】

New Class of Serine and Cysteine Protease Inhibitor with ChemotherapeuticPotential

机译:新一类具有化疗潜能的丝氨酸和半胱氨酸蛋白酶抑制剂

获取原文

摘要

Metastasis of cancer is dependent on a variety of biologically active compoundsincluding serine proteases. Inhibition of proteases such as plasmin is a potential route for both suppression of metastatic lesions and control of primary tumor growth. Synthesis of tetrahydrothiopyran-4-one based inhibitors of plasmin containing either a diamine or amide/amine side chain was undertaken. Initial attempts to produce the inhibitors through amide alkylation and reductive amination proved futile. The diamine inhibitor was finally produced using amine alkylation chemistry. A monoamine side product of this reaction forms the starting material for the other inhibitor. A simple peptide coupling reaction converts the monoamine to the amide/amine inhibitor. Preliminary testing on the crude products shows both inhibitors to have some activity against plasmin with a Ki of 6 mM for the diamine inhibitor and 3 mM for the amide/amine inhibitor.

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号