Inhibition of trypsin and urokinase by Cbz-amino(4-guanidinophenyl)methanephosphonate aromatic ester derivatives: the influence of the ester group on their biological activity |
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| Authors: | Sieńczyk Marcin Oleksyszyn Józef |
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| Institution: | 1. Department of Chemistry, Zhejiang University, Hangzhou 310027, China;2. Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang 310009, China;1. Institute of Health and Biomedical Innovation, Queensland University of Technology, Brisbane, Queensland, Australia;2. Laboratory of Genetic Skin Diseases, INSERM UMR 1163 and Imagine Institute of Genetic Diseases, Paris, France;3. Université Paris V Descartes—Sorbonne Paris Cité, Paris, France;4. Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland, Australia;5. Department of Medical Biosciences, Pathology, Umeå University, Umeå, Sweden;6. Australian Prostate Cancer Research Centre, Translational Research Institute, Brisbane, Queensland, Australia;7. Department of Genetics, Necker Hospital for Sick Children, Paris, France;1. State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China;2. Analytical & Testing Center, Sichuan University, Chengdu 610064, China;3. Sichuan Academy of Medical Science & Sichuan Provincial People’s Hospital, School of Medicine UESTC, Chinese Academy of Sciences Sichuan Translational Medicine Research Hospital, Chengdu 610072, China;1. Université de Tours, Tours, France;2. INSERM, UMR 1100, Research Center for Respiratory Diseases (CEPR), Team: “Proteolytic Mechanisms in Inflammation”, Tours, France;3. CNRS UPR 4301, Center for Molecular Biophysics (CBM), Team: “Molecular, Structural and Chemical Biology”, Orléans, France;4. Plateforme IBiSA de Microscopie Electronique, Université de Tours, Tours, France;5. Centre for Cancer Research and Cell Biology, School of Medicine, Dentistry and Biomedical Sciences, Queen''s University Belfast, Belfast, Northern Ireland, UK |
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| Abstract: | The urokinase plasminogen activator is a trypsin-like serine protease, important in tumor development. Here, we report the synthesis and biochemical evaluation of selective and potent diaryl esters of phosphonic-type inhibitors for urokinase. We have found that the substituted phenyl ester ring has a strong influence on the inhibitory activity of these compounds. This led to the most potent phosphonic inhibitor for uPA synthesized to date. |
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