Hits-to-Lead Optimization of the Natural Compound 2,4,6-Trihydroxy-3-geranyl-acetophenone (tHGA) as a Potent LOX Inhibitor: Synthesis, Structure-Activity Relationship (SAR) Study, and Computational Assignment

Hits-to-Lead Optimization of the Natural Compound 2,4,6-Trihydroxy-3-geranyl-acetophenone (tHGA) as a Potent LOX Inhibitor: Synthesis, Structure-Activity Relationship (SAR) Study, and Computational Assignment

A new series of 2,4,6-trihydroxy-3-geranyl-acetophenone (tHGA) analogues were synthesized and evaluated for their lipoxygenase (LOX) inhibitory activity. Prenylated analogues 4a–g (half maximal inhibitory concentration (IC50) values ranging from 35 μ M to 95 μ M) di...

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Bibliographic Details
Main Authors: Chean Hui Ng, Kamal Rullah, Faridah Abas, Kok Wai Lam, Intan Safinar Ismail, Fadzureena Jamaludin, Khozirah Shaari
Format: Article
Language:English
Published: MDPI AG 2018-09-01
Series:Molecules
Subjects:
Analogues
lipoxygenase
in-silico
ADMET
TOPKAT
Online Access:http://www.mdpi.com/1420-3049/23/10/2509

Internet

http://www.mdpi.com/1420-3049/23/10/2509

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