Marine microorganisms have been recognized as a new source for the production of bioactive secondary metabolites. The large numbers and diversity of marine bacteria suggest that this resource will be of significant importance in the discovery of new drugs.1 However, marine actinomycetes have been largely ignored until recently.2 As part of a continuing program to develop the biomedical potential of marine microorganisms, we have focused considerable attention on the marine actinomycetes. From the marine samples such as deep sea and shallow water sediments, plants and invertebrates, more than 4,000 strains of marine-derived actinomycetes were isolated. We have established that about 10% of isolates show some bioactivity in our assays such as cytotoxicity, antimicrobial, antifungal, and enzyme inhibitory activities. From the marine-derived isolates, several new actinomycetes have been identified and a variety of bioactive molecules were characterized. We present here the discovery of cytotoxic compounds from actinomycetes. The isolation, structure determination, and biological activity of new compounds from marine actinomycetes will be presented.