Title
Synthesis and evaluation of arylquinones as BACE1 inhibitors, β-amyloid peptide aggregation inhibitors, and destabilizers of preformed β-amyloid fibrils
Date Issued
15 April 2011
Access level
metadata only access
Resource Type
journal article
Author(s)
Ortega A.
Rincón A.
Bermejo-Bescós P.
Martín-Aragón S.
Molina M.T.
Csákÿ A.G.
Universidad Complutense
Abstract
BACE1 activity, inhibition of Aβ aggregation, and disaggregation of preformed Aβ fibrils constitute the three major targets in the development of small-molecule lipophilic new drugs for the treatment of Alzheimer's disease (AD). Quinones are widely distributed among natural products and possess relevant and varied biological activities including antitumor and antibiotic, inhibition of HIV-1 reverse transcriptase, antidiabetic, or COX-inhibition, among others. We report herein the interaction of several arylquinones and their derivatives with the amyloidogenic pathway of the amyloid precursor protein processing. Our studies put forward that these compounds are promising candidates in the development of new drugs which are effective simultaneously towards the three major targets of AD. © 2011 Elsevier Ltd. All rights reserved.
Start page
2183
End page
2187
Volume
21
Issue
8
Language
English
OCDE Knowledge area
Bioquímica, Biología molecular
Química medicinal
Scopus EID
2-s2.0-79953285877
PubMed ID
Source
Bioorganic and Medicinal Chemistry Letters
ISSN of the container
0960894X
Sponsor(s)
Andrea Ortega (PhD fellow) thanks the government of Chile and the ‘Universidad Católica del Norte’ (Antofagasta, Chile) for a grant (MECESUP program, UCN0604). Projects CTQ2009-14124-C02-01, CTQ2010-16170 and SAF2009-10399 from the Spanish government are gratefully acknowledged for financial support.
Sources of information:
Directorio de Producción Científica
Scopus