| Literature DB >> 26035340 |
Halesha D Basavarajappa1,2,3, Bit Lee4, Seung-Yong Seo4, Timothy W Corson1,2,3,5,6, Hyungjun Lee4, Rania S Sulaiman1,2,5,7, Hongchan An8, Carlos Magaña6, Mehdi Shadmand1,2, Alexandra Vayl1,2, Gangaraju Rajashekhar1,2, Eun-Yeong Kim9, Young-Ger Suh8, Kiho Lee9.
Abstract
Eye diseases characterized by excessive angiogenesis such as wet age-related macular degeneration, proliferative <span class="Disease">diabetic retinopathy, and retinopathy of prematurity are major causes of blindness. Cremastranone is an antiangiogenic, naturally occurring homoisoflavanone with efficacy in retinal and choroidal neovascularization models and antiproliferative selectivity for endothelial cells over other cell types. We undertook a cell-based structure-activity relationship study to develop more potent cremastranone analogues, with improved antiproliferative selectivity for retinal endothelial cells. Phenylalanyl-incorporated homoisoflavonoids showed improved activity and remarkable selectivity for retinal microvascular endothelial cells. A lead compound inhibited angiogenesis in vitro without inducing apoptosis and had efficacy in the oxygen-induced retinopathy model in vivo.Entities:
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Year: 2015 PMID： 26035340 PMCID： PMC4944207 DOI： 10.1021/acs.jmedchem.5b00449
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446