Synthesis and Evaluation of a Novel Nonsteroidal-Specific Endothelial Cell Proliferation Inhibitor

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, exemplifi...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2003-04, Vol.46 (8), p.1289-1292
Main Authors: Schmidt, Jonathan M, Tremblay, Gilles B, Pagé, Martine, Mercure, Julie, Feher, Miklos, Dunn-Dufault, Robert, Peter, Markus G, Redden, Peter R
Format: Article
Language:English
Subjects:
Angiogenesis Inhibitors - chemical synthesis
Angiogenesis Inhibitors - chemistry
Angiogenesis Inhibitors - pharmacology
Antineoplastic agents
Binding, Competitive
Biological and medical sciences
Cell Division - drug effects
Computer Simulation
Endothelium, Vascular - cytology
Endothelium, Vascular - drug effects
Estradiol - analogs & derivatives
Estradiol - chemistry
Estradiol - pharmacology
Estrogen Receptor alpha
Estrogen Receptor beta
General aspects
Humans
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Pyrans - chemical synthesis
Pyrans - chemistry
Pyrans - pharmacology
Receptors, Estrogen - metabolism
Structure-Activity Relationship
Tumor Cells, Cultured
Umbilical Veins - cytology
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm034007d