Department of Medicinal Chemistry, Drug and Biomaterial R&D, Genzyme Corporation, Waltham, MA 02451, USA.
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4550-4. doi: 10.1016/j.bmcl.2010.06.019. Epub 2010 Jun 17.
Building on our initial work, we have identified additional novel inhibitors of sphingosine kinase-1 (SK1). These new analogs address the shortcomings found in our previously reported compounds. Inhibitors 51 and 54 demonstrated oral bioavailability in a rat PK study.
在我们初步工作的基础上,我们又鉴定了一些新的丝氨酸激酶-1(SK1)的抑制剂。这些新的类似物解决了我们之前报道的化合物存在的缺陷。抑制剂 51 和 54 在大鼠 PK 研究中表现出了口服生物利用度。