Synthesis and SAR studies of mono O-prenylated coumarins as potent 15-lipoxygenase inhibitors

…, R Mehri, S Zeraatkar, T Ahmadi, M Alimardani…

文献索引：Iranshahi, Mehrdad; Jabbari, Atena; Orafaie, Ala; Mehri, Robabeh; Zeraatkar, Soudabeh; Ahmadi, Taraneh; Alimardani, Maliheh; Sadeghian, Hamid European Journal of Medicinal Chemistry, 2012 , vol. 57, p. 134 - 142

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被引用次数: 24

摘要

All of the mono isopentenyloxy,-geranyloxy and-farnesyloxy derivatives of coumarin were synthesized and their inhibitory potency against soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (HLO-1) were determined. Amongst the synthetic analogs, 5- farnesyloxycoumarin showed the most potent inhibitory activity against SLO (IC50= 0.8 μM) while 6-farnesyloxycoumarin was the strongest HLO-1 inhibitor (IC50= 1.3 μM). The IC50 ...