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 (IC(50)) values ranging from 35 μM to 95 μM) did not exhibit better inhibitory ac...

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Detalles Bibliográficos
Autores principales: Ng, Chean Hui, Rullah, Kamal, Abas, Faridah, Lam, Kok Wai, Ismail, Intan Safinar, Jamaludin, Fadzureena, Shaari, Khozirah
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222424/
https://www.ncbi.nlm.nih.gov/pubmed/30274341
http://dx.doi.org/10.3390/molecules23102509

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222424/
https://www.ncbi.nlm.nih.gov/pubmed/30274341
http://dx.doi.org/10.3390/molecules23102509

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