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

• Main Authors: Ng, Chean Hui, Rullah, Kamal, Abas, Faridah, Lam, Kok Wai, Ismail, Intan Safinar, Jamaludin, Fadzureena, Shaari, Khozirah
• Format: Article
• Published: MDPI 2018
• Subjects: Q Science (General); R Medicine
• Online Access: http://eprints.um.edu.my/21149/; https://doi.org/10.3390/molecules23102509

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 μM to 95 μM) did not exhibit better inhibitory acti...