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) did not exhibit better inhibitory ac...

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Bibliographic Details

Main Authors:	Ng, Chean Hui, Rullah, Kamal, Abas, Faridah, Lam, Kok Wai, Ismail, Intan Safinar, Jamaludin, Fadzureena, Shaari, Khozirah
Format:	Article
Language:	en
Published:	MDPI 2018
Subjects:	RS403 Materia Medica-Pharmaceutical Chemistry
Online Access:	http://irep.iium.edu.my/74949/1/Kamal%20Rullah%2020.pdf http://irep.iium.edu.my/74949/ https://www.mdpi.com/1420-3049/23/10/2509/htm
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