期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 47, 期 -, 页码 351-359出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.11.003
关键词
4-(Benzyloxy)-1-phenylbut-2-yn-1-ol derivatives; 5-LOX; Site point connection method; In silica prediction; Carcinoma cell line; Acute lung injury
资金
- UGC
- DBT-RA
- CSIR
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 IC50 value of 8 mu M 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). (C) 2011 Elsevier Masson SAS. All rights reserved.
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