Synthesis and biological evaluation of analogs of the marine toxin polycavernoside A

Second generation analogs of polycavernoside A (2) possessing a side chain at C-15 different from that of the natural toxin have been synthesized. The in vivo toxicities of these new compounds (expressed as the minimal lethal dose) have been evaluated in mice (ip) and compared to 2, its aglycone (8), and polycavernoside B (9). The bioactivity profile of enynene 5 is particularly notable.