D. Castagna, Emma L. Duffy, Dima Semaan
Jun 10, 2015
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0
Influential Citations
5
Citations
Journal
MedChemComm
Abstract
Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1antagonists led us to the discovery of three novel series of inhibitors of the ectoenzyme autotaxin (ATX), responsible for LPA production in blood, with potencies in the range of 1–4 μM together with good (>100 μg mL−1) solubility.