Cortistatins

blocks_imageThe cortistatins are a family of anti-angiogenic alkaloids that were isolated from the marine sponge Corticium simplex. Several of these compounds exhibit extremely potent (2 – 40 nM) and selective cytostatic activity against human umbilical vein endothelial cells (HUVECs) with markedly less potency against normal human dermal fibroblasts (NHDFs) and a panel of human cancer cell lines (including KB3-1, Neuro2A, and K562). We have recently developed an efficient and scalable synthesis of cortistatins A, J, K, and L from which we can access a large number of diverse cortistatin derivatives for use in antiproliferative assays and in target-identification studies, which figure prominently in our current research.