2. Academic Validation
  3. Synthesis and Biological Evaluation of Novel Homoisoflavonoids for Retinal Neovascularization

Synthesis and Biological Evaluation of Novel Homoisoflavonoids for Retinal Neovascularization

  • J Med Chem. 2015 Jun 25;58(12):5015-5027. doi: 10.1021/acs.jmedchem.5b00449.
Halesha D Basavarajappa # 1 2 3,  Bit Lee # 4,  Hyungjun Lee 4,  Rania S Sulaiman 1 2 5 6,  Hongchan An 7,  Carlos Magaña 8,  Mehdi Shadmand 1 2,  Alexandra Vayl 1 2,  Gangaraju Rajashekhar 1 2,  Eun-Yeong Kim 9,  Young-Ger Suh 7,  Kiho Lee 9,  Seung-Yong Seo # 4,  Timothy W Corson # 1 2 3 5 8
Affiliations

Affiliations

  • 1 Eugene and Marilyn Glick Eye Institute, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
  • 2 Department of Ophthalmology, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
  • 3 Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
  • 4 College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 406-840, South Korea.
  • 5 Department of Pharmacology and Toxicology, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
  • 6 Department of Biochemistry, College of Pharmacy, Cairo University, Cairo, Egypt.
  • 7 College of Pharmacy, Seoul National University, Seoul, South Korea.
  • 8 Melvin and Bren Simon Cancer Center, Indiana University School of Medicine, Indianapolis, Indiana 46202, United States.
  • 9 College of Pharmacy, Korea University, Sejong, South Korea.
  • # Contributed equally.
PMID: 26035340 DOI: 10.1021/acs.jmedchem.5b00449
Abstract

Eye diseases characterized by excessive angiogenesis such as wet age-related macular degeneration, proliferative 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.

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