Euodenine A: a small-molecule agonist of human TLR4

…, G Nikolakopoulos, PV Le, P de A. Leone…

Index: Neve, Juliette E.; Wijesekera, Hasanthi P.; Duffy, Sandra; Jenkins, Ian D.; Ripper, Justin A.; Teague, Simon J.; Campitelli, Marc; Garavelas, Agatha; Nikolakopoulos, George; Le, Phuc V.; De A. Leone, Priscila; Pham, Ngoc B.; Shelton, Philip; Fraser, Neil; Carroll, Anthony R.; Avery, Vicky M.; McCrae, Christopher; Williams, Nicola; Quinn, Ronald J. Journal of Medicinal Chemistry, 2014 , vol. 57, # 4 p. 1252 - 1275

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Citation Number: 10

Abstract

A small-molecule natural product, euodenine A (1), was identified as an agonist of the human TLR4 receptor. Euodenine A was isolated from the leaves of Euodia asteridula (Rutaceae) found in Papua New Guinea and has an unusual U-shaped structure. It was synthesized along with a series of analogues that exhibit potent and selective agonism of the TLR4 receptor. SAR development around the cyclobutane ring resulted in a 10-fold ...