Design and Synthesis of Marine Phidianidine Derivatives as Potential Immunosuppressive Agents

A series of novel marine phidianidine
derivatives were designed,
synthesized, and evaluated for their immunosuppressive activities
during our search of potential immunosuppressive agents with high
efficacy and low toxicity from marine sources. These compounds were
tested for their inhibitory activity on Con A-induced T cell and lipopolysaccharide-induced
B cell proliferation. Compounds 14a and 18c, displaying the most promising inhibitory effects and low toxicities,
were further found to possess immune-regulatory activities upon cross-linking
of T cell receptor (TCR) and B cell receptor (BCR) on purified T and
B cells, respectively.