Total synthesis and antimalarial activity of symplostatin 4

Article abstract of DOI:10.1021/ol1024663

The first total synthesis of symplostatin 4, a marine cyanobacterium- derived natural product, is described. Notable features of the route include the efficient preparation of three key fragments and final assembly to the natural product via sequential imide and amide couplings. Symplostatin 4 was also demonstrated to possess significant antimalarial activity (ED₅₀ of 74 nM against Plasmodium falciparum, strain 3D7).