Lee, Bit; Sun, Wei; Lee, Hyungjun; Basavarajappa, Halesha; Sulaiman, Rania S.; Sishtla, Kamakshi; Fei, Xiang; Corson, Timothy W.; Seo, Seung-Yong published the artcile< Design, synthesis and biological evaluation of photoaffinity probes of antiangiogenic homoisoflavonoids>, Category: esters-buliding-blocks, the main research area is photoaffinity probe antiangiogenic homoisoflavonoid; Antiangiogenic agents; Homoisoflavonoids; Human retinal microvascular endothelial cells; Photoaffinity probes; Wet age-related macular degeneration.
A naturally occurring homoisoflavonoid cremastranone (1) inhibited angiogenesis in vitro and in vivo. The authors developed an analog SH-11037 (2) which is more potent than cremastranone in human retinal microvascular endothelial cells (HRECs) and blocks neovascularization in animal models. Despite their efficacy, the mechanism of these compounds is not yet fully known. In building on a strong foundation of SAR and creating a novel chem. tool for target identification of homoisoflavonoid-binding proteins, various types of photoaffinity probes were designed and synthesized in which benzophenone and biotin were attached to homoisoflavanonoids using PEG linkers on either the C-3′ or C-7 position. Notably, the photoaffinity probes linking on the phenol group of the C-3′ position retain excellent activity of inhibiting retinal endothelial cell proliferation with up to 72 nM of GI50.
Bioorganic & Medicinal Chemistry Letters published new progress about Antiangiogenic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.
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