AI Article Synopsis
- A series of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives were created and tested for their ability to inhibit the enzyme 5-Lipoxygenase (5-LOX), using a method that focused on targeting hydrophobic areas of the enzyme.
- Among the compounds, 4k showed significant inhibitory activity against 5-LOX with an IC(50) value of 8 μM, and both 4j and 4k demonstrated strong cytotoxic effects on multiple cancer cell lines without harming normal cells.
- Additionally, 4k provided protective effects in a mouse model of Acute Lung Injury, suggesting its potential as a therapeutic agent
Article Abstract
A group of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives were designed using Site point connection method, synthesized and evaluated for their 5-Lipoxygenase (5-LOX) inhibitory activity. Hydrophobic site points in 5-LOX were considered for the study and substitutions were planned such that 4k will have strong hydrophobic group in the corresponding site point. Biological results supported the in silico prediction with compound 4k exhibiting good inhibition with IC(50) value of 8 μM against 5-LOX. The compounds 4j and 4k showed potent cytotoxic effects against various cancer cell lines (COLO-205, MDA-MB-231 and HepG2) but with no effect on normal cell line (HaCaT). The overall trend showed 4k as the most potent compound. Further studies demonstrated the protective effect of 4k in mouse Acute Lung Injury (ALI) model induced by lipopolysaccharide (LPS).
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| http://dx.doi.org/10.1016/j.ejmech.2011.11.003 | DOI Listing |
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