4.8 Article

Synthesis of Denosomin-Vitamin D3 Hybrids and Evaluation of Their Anti-Alzheimer's Disease Activities

Journal

ORGANIC LETTERS
Volume 17, Issue 23, Pages 5910-5913

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b03138

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Funding

  1. KAKENHI [25460010]
  2. Grants-in-Aid for Scientific Research [25460010] Funding Source: KAKEN

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As an extension of previously conducted studies on developing an anti-Alzheimer's disease agent, denosomin (1-deoxy-24-norsominone, an artificial inducer of neurite elongation), derivatives were designed and synthesized based on the hypothesis that our denosomin would exhibit axonal extension activity via a 1,25D(3)-membrane-associated, rapid response steroid-binding protein (1,25D(3)-MARRS) pathway. The biological assay revealed that the hybridization of characteristic delta-lactone in denosomin and the triene moiety in VD3 was effective to enhance the nerve re-extension activity in amyloid beta (A beta)-damaged neurons.

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