FE399

FE399 is a novel bicyclic cyclic depsipeptide originally isolated as an antitumor antibiotic from a filamentous fungus of the genus Ascochyta and later fully synthesized using MNBA-mediated macrolactamization chemistry.[4][7][10] Structurally, it is a 16-membered macrolactam-based bicyclic depsipeptide containing two cysteine residues that form an intramolecular disulfide bridge, and it exists as a mixture of conformational isomers in solution.[1][6][7] Biologically, FE399 exhibits potent anticancer activity in vitro against a wide range of human cancer cell lines, particularly colorectal cancer, by inducing apoptosis through reactivation of intrinsic “self-destruct” pathways in tumor cells, with promising in vivo antitumor effects in xenograft models.[4][6][8][11] Because natural production and purification from the fungal source are challenging, current work focuses on total synthesis and analogue generation as leads for future anticancer drug development, but FE399 itself remains at the preclinical research stage without clinical development. [4][5][7]

Other names

antitumor antibiotic FE399cyclic depsipeptide FE399bicyclic depsipeptide FE399