Alpha- and Beta-substituted Phosphonate Analogs of LPA As Autotaxin Inhibitors

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2007 Dec 18

PMID 18082408

Citations 13

Authors

Peng Cui

William F McCalmont

Jose L Tomsig

Kevin R Lynch

Timothy L Macdonald

Affiliations

Soon will be listed here.

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.

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