12-epi-scalarin and Leukemia-P388

Novel scalarane sesterterpenes (1-4) were isolated from a sponge, Hyrtios erecta (order Dictyoceratida). They were characterized by means of spectral analyses, X-ray crystallography, and chemical reactions. Compound 1 showed potent in vitro and in vivo antitumor activities. In addition, the structure-activity relationship was also discussed using computer-assisted structure matching of 1 and aragusterols.

Topics: Animals; Antineoplastic Agents; Crystallography, X-Ray; Drug Screening Assays, Antitumor; Leukemia P388; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Molecular Conformation; Plant Extracts; Porifera; Sesterterpenes; Spectrophotometry, Infrared; Spectrophotometry, Ultraviolet; Structure-Activity Relationship; Terpenes; Tumor Cells, Cultured