The spiroxins (1-5) were purified from the culture extract of a marine-derived fungus. Their unique bisnaphthospiroketal structures were established by NMR spectroscopy. In addition to cytotoxicity, these compounds showed antibiotic activity and were active in a mouse xenograft model against human ovarian carcinoma. The mechanism of action of these compounds was shown to be due, in part, to their effect on DNA. (C) 1999 Elsevier Science Ltd. All rights reserved.