Journal
MEDICINAL CHEMISTRY
Volume 9, Issue 2, Pages 303-311Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1573406411309020013
Keywords
Halophenols; furan-2-yl(phenyl)methanone; protein tyrosine kinase (PTK) inhibitor; vascular smooth muscle cell (VSMC) proliferation inhibitor; Structure-activity relationships (SAR)
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Funding
- State 863 Projects of China [2013]
- National Natural Science Foundation of China [81172938]
- Shanxi Foundation for overseas returned
- Program for the Top Young and Middle-aged Innovative Talents of Higher Learning Institutions of Shanxi Province
- Program for the Top Science and Technology Innovation Teams of Higher Learning Institutions of Shanxi province
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A series of new halophenols were synthesized, and their structures were established on the basis of 1 H, 13 C NMR and mass spectral data. All of the prepared compounds were screened for their in vitro protein tyrosine kinase (PTK) and vascular smooth muscle cell (VSMC) proliferation inhibitory activity. Twelve halophenols showed significant PTK inhibitory activity, most of them exhibited stronger activities than that of genistein, a positive reference compound. Several halophenols also displayed moderate VSMC proliferation inhibitory activity, compound 8c showed higher activity than that of tetrandrine, a positive reference compound. The preliminary structure-activity relationships of these compounds were investigated and discussed. The results provided a foundation for the action mechanism study and further structure optimization of the halophenols.
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