4.7 Article

Tunable regulatory activities of 1,10-phenanthroline derivatives towards acid sphingomyelinase and Zn(II)-amyloid-β

Journal

CHEMICAL COMMUNICATIONS
Volume 55, Issue 42, Pages 5847-5850

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c9cc01005j

Keywords

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Funding

  1. National Research Foundation of Korea (NRF) - Korean government [NRF-2016R1A5A1009405, NRF-2017R1A2B3002585, NRF-2017R1A4A1015652, NRF-2018M3C7A1056513]
  2. KAIST
  3. Korea Health Technology R&D Project through the KHIDI - Ministry of Health & Welfare, Republic of Korea [HI16C2131]
  4. National Research Foundation of Korea [2018M3C7A1056513] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

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We report a new series of small molecules able to achieve the tunability of modulatory activities against acid sphingomyelinase (ASM) and Zn(II)bound amyloid-beta [ Zn(II)-A beta], two pathological targets found in the brain affected by Alzheimer's disease. Rational tuning of the hydrophobicity and Zn(II) binding affinity of the 1,10-phenanthroline (phen) framework successfully yielded compounds as chemical modulators for ASM (4 and 5), Zn(II)-A beta (phen, 1, and 2), or both (3).

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