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Small-Molecule Inhibitors of Angiogenesis

Angiogenesis, the growth of new blood vessels from existing vessels, is a normal and vital process in growth and development. Deregulation of angiogenesis plays a role in many human diseases, including cancer, age-related macular degeneration, diabetic retinopathy, and endometriosis.

National Cancer Institute investigators have used a cell-based high-throughput screening method to identify a set of anti-angiogenic small molecules. These compounds are highly active, inhibiting both endothelial cell growth and tube formation, and are not cytotoxic. Structure-activity relationship analysis has revealed that these compounds are unrelated to known anti-angiogenic compounds, and hence may operate through a novel mechanism of action. Thus, these compounds would be promising candidates for the development of new anti-angiogenesis therapeutics.

Applications Development of new anti-angiogenesis therapeutics.

Advantages: These compounds are structurally unrelated to other known anti-angiogenesis compounds, and exhibit high activity without cytotoxicity.

Development Status: In vivo studies using xenograft models are underway.

More info: Tara Kirby, Ph.D.; 301-435-4426; tarak@mail.nih.gov