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Synthesis and evaluation of a novel nonsteroidal-specific endothelial cell proliferation inhibitor.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2003 Apr 10; Vol. 46 (8), pp. 1289-92. - Publication Year :
- 2003
-
Abstract
- The identification of agents with specific antiproliferative or cytostatic activity against endothelial cells has significant value for the treatment of pathologies associated with angiogenesis, including solid tumors. Here, we describe a novel substituted dibenzo[b,d]pyran-6-one scaffold, exemplified by structures 9a and 10, and report preliminary in vitro activity data indicating that this scaffold is a promising lead for the development of specific inhibitors of endothelial cell proliferation.
- Subjects :
- 2-Methoxyestradiol
Angiogenesis Inhibitors chemistry
Angiogenesis Inhibitors pharmacology
Binding, Competitive
Cell Division drug effects
Computer Simulation
Endothelium, Vascular cytology
Estradiol analogs & derivatives
Estradiol chemistry
Estradiol pharmacology
Estrogen Receptor alpha
Estrogen Receptor beta
Humans
Models, Molecular
Pyrans chemistry
Pyrans pharmacology
Receptors, Estrogen metabolism
Structure-Activity Relationship
Tumor Cells, Cultured
Umbilical Veins cytology
Angiogenesis Inhibitors chemical synthesis
Endothelium, Vascular drug effects
Pyrans chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 46
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 12672229
- Full Text :
- https://doi.org/10.1021/jm034007d