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ID: ALA1142314

Journal: Bioorg Med Chem

Title: alpha- and beta-substituted phosphonate analogs of LPA as autotaxin inhibitors.

Authors: Cui P, McCalmont WF, Tomsig JL, Lynch KR, Macdonald TL.

Abstract: Autotaxin (ATX) is an attractive pharmacological target due to its lysophospholipase D activity which leads to the production of lysophosphatidic acid (LPA). Blockage of ATX produced LPA by small molecules could be a potential anticancer chemotherapy. In our previous study, we have identified the two beta-hydroxy phosphonate analogs of LPA (compounds f17 and f18) as ATX inhibitors. With this work, we investigated alpha- and beta-substituted phosphonate analogs of LPA and evaluated them for ATX inhibitory activity. The stereochemistry of beta-hydroxy phosphonates was also studied.

CiteXplore: 18082408

DOI: 10.1016/j.bmc.2007.11.078