α- and β-Substituted phosphonate analogs of LPA as autotaxin inhibitors
α- and β-Substituted phosphonate analogs of LPA as autotaxin inhibitors
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DOI：
10.1016/j.bmc.2007.11.078
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发表时间：
2008-03-01
影响因子：
3.5
通讯作者：
Macdonald, Timothy L.
中科院分区：
文献类型：
--
作者：
Cui, Peng;McCalmont, William F.;Macdonald, Timothy L.
自分泌运动因子（ATX）由于其溶血磷脂酶D活性导致溶血磷脂酸（LPA）的产生而成为有吸引力的药理学靶标。小分子药物阻断ATX产生的LPA可能成为一种潜在的抗肿瘤化疗药物。在我们先前的研究中，我们已经鉴定了LPA的两种β-羟基膦酸酯类似物（化合物f17和f18）作为ATX抑制剂。通过这项工作，我们研究了LPA的α-和β-取代的膦酸酯类似物，并评估了它们的ATX抑制活性。还研究了β-羟基膦酸酯的立体化学。爱思唯尔有限公司出版
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. Published by Elsevier Ltd.