Angiogenesis, the formation of new blood vessels from pre-existing host vasculatures stimulated by biochemical stimulators, is involved in wound healing, embryonic development, and the female reproductive cycle, which is under elaborate regulations in normal vascular system.1 However, malignant angiogenesis plays a critical role in several fatal diseases including cancer, vascular insufficiency, diabetic retinopathy, and rheumatoid arthritis by a normal delivering mechanism of oxygen and nutrients to cell and tissue. Because tumor angiogenesis caused by angiogenic inducers is the most critical factor in the growth of solid tumors,2 as well as their invasion and metastasis,3 early control of angiogenesis may be a promising therapeutic strategy for the related diseases.4 As part of our ongoing program to develop the biomedical potential of marine microorganisms, we have focused considerable attention on the marine actinomycetes. From the bioactive isolates several new actinomycetes have been identified and a variety of bioactive molecules were characterized. We present here the discovery of anti-angiogenesis compounds from marine-derived actinomycetes. The isolation, structure determination, and anti-angiogenesis activity of the compounds from marine actinomycetes will be presented.