期刊
DRUG DEVELOPMENT RESEARCH
卷 73, 期 6, 页码 343-351出版社
WILEY-BLACKWELL
DOI: 10.1002/ddr.21038
关键词
metrix metalloproteinase; caffeic acid; tumor; structure-activity relationship
资金
- National Natural Science Foundation of China [81001382, 81274058]
- Program for New Century Excellent Talents by the Ministry of Education [NCET-09-0163]
- Research Fund for the Doctoral Program of Higher Education of China [20093237120012]
- Main Training Fund of Nanjing University of Chinese Medicine [10XPY02]
- 33 High-Level Talents Training Project
- Jiangsu Province, Six Talents Project
- Jiangsu Province [2011-D-078]
- Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education
- Key Research Project in Basic Science of Jiangsu College and University [06KJA36022, 07KJA36024, 10KJA360039]
- Priority Academic Program Development of Jiangsu Higher Education Institutions [ysxk-2010]
- Construction Project for Jiangsu Engineering Center of Innovative Drug from Blood-Conditioning TCM Formulae
Strategy, Management and Health Policy Preclinical Research A series of caffeic acid amides with extended P1' groups were synthesized and tested for their inhibitory activities on matrix metalloproteinase (MMP)-1, MMP-2, and MMP-9. Compound 3f showed considerable inhibitory activities against MMP-2, MMP-9, and best selectivity over MMP-1. Preliminary structureactivity relationship analysis and docking studies indicated that caffeic acid amides with electron-donating groups at p-position of amino phenyl group showed better inhibitory activities and selectivity than those with electron-withdrawing groups. The findings of this study would provide information for the exploitation and utilization of caffeic acid as MMP inhibitor for metastatic tumor treatment.
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