Discovery of Direct Growth Inhibition of Various Types of Cancer Cells by Fusarochromanone

This invention offers promise for the treatment of cancer and angiogenic diseases, including arthritis.

Angiogenis is the development of new blood vessels from existing capillaries. While the process normally develops healthy new blood vessels, it can be a factor in a number of human diseases, including the growth and metastasis of tumors and arthritis. In some forms of arthritis, new capillaries form in the joint, leading to its gradual destruction. Solid tumors also must stimulate the formation of new blood vessels in order to obtain the nutrients and oxygen that are necessary for their growth, and thus, angiogenesis can provide a route by which the tumors can metastasize to distant sites. Therefore, development of biologically active agents that inhibit angiogenesis is highly desirable because of their potential in providing effective treatment for cancer, arthritis, and other angiogenic diseases.

The invention provides a treatment for angiogenic diseases in humans and animals. It is a small molecular weight, orally available compound that strongly inhibits tumor growth by acting in two ways. The compound shows potent anti-cancer activity against a variety of human tumor cells, while maintaining low toxicity to normal cells. The compound is also effective in inhibiting angiogenesis, which makes it effective in helping to stop the spread of tumors. This unique combination of anti-cancer activity and anti-angiogenic activity makes this compound attractive for clinical development. Furthermore, the compound has favorable pharmacokinetic properties with an in vivo half-life of over 12 hours. The purification process to isolate the highly pure compound from the natural source for preclinical studies has been optimized.