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 (<b>1</b>) and <i>p</i>-hydroxy-cinnamic acid (<b>2</b>), were subjected to systematic structure modifications, including various positions in luteolin segment for conjugation, different linke...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/25/1/102 |
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| author | De-Yang Sun Chen Cheng Katrin Moschke Jian Huang Wei-Shuo Fang |
| author_facet | De-Yang Sun Chen Cheng Katrin Moschke Jian Huang Wei-Shuo Fang |
| author_sort | De-Yang Sun |
| collection | DOAJ |
| description | BACE1 inhibitory conjugates derived from two natural products, luteolin (<b>1</b>) and <i>p</i>-hydroxy-cinnamic acid (<b>2</b>), 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 <b>7c</b> and <b>7k</b> were chosen on the basis of a series of bioassay data for further investigation. |
| first_indexed | 2024-12-10T21:17:21Z |
| format | Article |
| id | doaj.art-60a0f428952848d180e655269319d580 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-10T21:17:21Z |
| publishDate | 2019-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-60a0f428952848d180e655269319d5802022-12-22T01:33:15ZengMDPI AGMolecules1420-30492019-12-0125110210.3390/molecules25010102molecules25010102Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological PropertiesDe-Yang Sun0Chen Cheng1Katrin Moschke2Jian Huang3Wei-Shuo Fang4State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2A Nan Wei Road, Beijing 100050, ChinaCollege of Life Science, Wuhan University, Wuhan 430072, Hubei, ChinaGerman Center for Neurodegenerative Diseases (DZNE) and Munich Cluster for Systems Neurology (SyNergy), Technical University of Munich, Feodor-Lynen-Strasse 17, 81377 Munich, GermanyCollege of Life Science, Wuhan University, Wuhan 430072, Hubei, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2A Nan Wei Road, Beijing 100050, ChinaBACE1 inhibitory conjugates derived from two natural products, luteolin (<b>1</b>) and <i>p</i>-hydroxy-cinnamic acid (<b>2</b>), 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 <b>7c</b> and <b>7k</b> were chosen on the basis of a series of bioassay data for further investigation.https://www.mdpi.com/1420-3049/25/1/102beta-secretasebace1 inhibitorflavonoidluteolincinnamic acid |
| spellingShingle | De-Yang Sun Chen Cheng Katrin Moschke Jian Huang Wei-Shuo Fang Extensive Structure Modification on Luteolin-Cinnamic Acid Conjugates Leading to BACE1 Inhibitors with Optimal Pharmacological Properties Molecules beta-secretase bace1 inhibitor flavonoid luteolin cinnamic acid |
| 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 | beta-secretase bace1 inhibitor flavonoid luteolin cinnamic acid |
| url | https://www.mdpi.com/1420-3049/25/1/102 |
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