diazepinomicin

Diazepinomicin (TLN-4601) is a structurally novel farnesylated dibenzodiazepinone discovered using Thallion Pharmaceuticals' DECIPHER drug discovery platform. It is a small molecule with antineoplastic activity that inhibits the Ras/RAF/MAPK signaling pathway by inducing proteasomal degradation of Raf-1 protein and preventing downstream phosphorylation events in the pathway. Diazepinomicin also selectively binds to the peripheral benzodiazepine receptor (translocator protein/TSPO), which may contribute to tumor-specific accumulation and apoptosis induction in certain cancer cells. The compound has demonstrated broad cytotoxic activity across various tumor cell lines and can cross the blood-brain barrier. Clinical development included phase I and II trials for glioblastoma multiforme (GBM), but further development was discontinued due to lack of efficacy[1][2][3][4][5][6][7][8].

Other names

diazepinomicin4,6,8-trihydroxy-10-(3,7,11-trimethyldodeca-2,6,10-trienyl)-5,10-dihydrodibenzo(b,e)(1,4)diazepin-11-one