期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 -, 页码 74-84出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.07.003
关键词
Filifolinol derivatives; C-7 Functionalization; Complement inhibitors; Classical pathway; K-76 COOH analogs; Pd-Catalyzed C-C bond formation
资金
- Argentine National Research Council (CONICET) [3294]
- National Agency for Promotion of Science and Technology (ANPCyT) [PICT 06-13865]
- Secretary of Science and Technology of the National University of Rosario (SECyT-UNR)
A series of carboxylic acids carrying various functionalization on C-7 of their common 3H-spiro [benzofuran-2,1'-cyclohexane] skeleton were synthesized from filifolinol, as analogs of the natural Complement inhibitor K-76 COOH. In order to probe the relevance of the C-7 functionalization on their bioactivity, the ability of the analogs to inhibit Complement activation through the classical pathway was determined. The observed results suggest that functionalization of C-7 can modulate the inhibitory activity of the tested compounds. The 7-trifluoromethyl derivative was the compound with the lowest IC50 value among the tested analogs (IC50 = 100 mu M), being more potent than K-76 COOH (IC50 = 570 mu M). (C) 2012 Elsevier Masson SAS. All rights reserved.
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