Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties

BACE1 inhibitory conjugates derived from two natural products, luteolin (1) and p-hydroxy-cinnamic acid (2), were subjected to systematic structure modifications, including various positions in luteolin segment for conjugation, different linkers (length, bond variation), as well as various substitut...

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Autores principales: Sun, De-Yang, Cheng, Chen, Moschke, Katrin, Huang, Jian, Fang, Wei-Shuo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6982702/
https://www.ncbi.nlm.nih.gov/pubmed/31888099
http://dx.doi.org/10.3390/molecules25010102
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author Sun, De-Yang
Cheng, Chen
Moschke, Katrin
Huang, Jian
Fang, Wei-Shuo
author_facet Sun, De-Yang
Cheng, Chen
Moschke, Katrin
Huang, Jian
Fang, Wei-Shuo
author_sort Sun, De-Yang
collection PubMed
description BACE1 inhibitory conjugates derived from two natural products, luteolin (1) and p-hydroxy-cinnamic acid (2), were subjected to systematic structure modifications, including various positions in luteolin segment for conjugation, different linkers (length, bond variation), as well as various substitutions in cinnamic acid segment (various substituents on benzene, and replacement of benzene by heteroaromatics and cycloalkane). Optimal conjugates such as 7c and 7k were chosen on the basis of a series of bioassay data for further investigation.
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spelling pubmed-69827022020-02-28 Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties Sun, De-Yang Cheng, Chen Moschke, Katrin Huang, Jian Fang, Wei-Shuo Molecules Article BACE1 inhibitory conjugates derived from two natural products, luteolin (1) and p-hydroxy-cinnamic acid (2), were subjected to systematic structure modifications, including various positions in luteolin segment for conjugation, different linkers (length, bond variation), as well as various substitutions in cinnamic acid segment (various substituents on benzene, and replacement of benzene by heteroaromatics and cycloalkane). Optimal conjugates such as 7c and 7k were chosen on the basis of a series of bioassay data for further investigation. MDPI 2019-12-26 /pmc/articles/PMC6982702/ /pubmed/31888099 http://dx.doi.org/10.3390/molecules25010102 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sun, De-Yang
Cheng, Chen
Moschke, Katrin
Huang, Jian
Fang, Wei-Shuo
Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
title Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
title_full Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
title_fullStr Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
title_full_unstemmed Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
title_short Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties
title_sort extensive structure modification on luteolin-cinnamic acid conjugates leading to bace1 inhibitors with optimal pharmacological properties
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6982702/
https://www.ncbi.nlm.nih.gov/pubmed/31888099
http://dx.doi.org/10.3390/molecules25010102
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