3-[1-(3-Hydroxy-4-methoxyphenyl)-meth-(E)-ylidene]-6-methyl-chroman-4-one

An anti-proliferative and anti-angiogenic compound. IMS2186 is a novel synthetic compound developed as an anti-CNV drug. The proposed mechanism of action under investigation, is blocking the cell cycle at G2 and inhibiting the production of PGE2/TNF-. The latter contributing to anti-angiogenic and antiinflammatory effects. IMS2186 inhibits cell growth in vitro in tumor cells, non-transformed fibroblasts, and retinal pigment epithelial cells. IMS2186 inhibits angiogenesis (IC50= 0.1 M) and cell migration, which plays a role in many biological processes: inflammation, angiogenesis, and scar formation. The physicochemical structure of IMS2186 showed also that the free drug concentration in a physiological media (e.g., vitreous or saline) is 8-10 M above the IC50 for all these activities (0.1-3.0 M). Intraocular injection of IMS2186 could be a long-lasting effective treatment for CNV (choroidal neovascularization) in AMD (age-related macular degeneration) with a reduction in scarring and related visual loss.