Synthesis of N-Heteroaroyl Aminosaccharide Derivatives as Fibroblast Growth Factor 2 Signaling Modulators

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概要

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• Fibroblast growth factor 2 (FGF2) signaling plays an important role in angiogenesis. Heparin/heparan sulfate (HS) is required for FGF2 signaling but heparin mimics either promotes or inhibits FGF2 signaling. To take advantage such properties of heparin mimics, a series of N-heteroaroyl aminosaccharide derivatives were designed and synthesized as FGF2 signaling modulators. The bioactivity was determined in a FGF2 and heparin-dependent cell proliferation assay using FGFR1c expressing BaF3 cells. We found that most of the compounds inhibited heparin- and FGF2-dependent BaF3 cell proliferation while three compounds promoted the cell proliferation. These results suggest that the small molecular heparin mimics approach might be useful in developing novel anti-angiogenic agents.

著者

• Dong Jin

  Department of Chemical Pharmaceutics, Shenyang Pharmaceutical University

• Yao Shuowei

  Department of Medicinal Chemistry, China Pharmaceutical University

• Zhou Xiaodong

  Department of Pathology and Immunology, Washington University School of Medicine

• Zhang Lijuan

  Department of Pathology and Immunology, Washington University School of Medicine

• Xu Yungen

  Department of Medicinal Chemistry, China Pharmaceutical University

• Dong Jin

  Department of Medicinal Chemistry, China Pharmaceutical University

関連論文

• Synthesis of N-Heteroaroyl Aminosaccharide Derivatives as Fibroblast Growth Factor 2 Signaling Modulators
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