Institute of Organic Chemistry and Biochemistry, v.v.i., Gilead Sciences & IOCB Research Center, Academy of Sciences of the Czech Republic, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.
Bioorg Med Chem Lett. 2011 Jan 15;21(2):652-4. doi: 10.1016/j.bmcl.2010.12.027. Epub 2010 Dec 10.
3- and 8-(8-phosphonooctyl)-8-aza-7,9-dideazaxanthine, and 1,8-bis(8-aza-7,9-dideazaxanthin-8-yl)octane were prepared and found to inhibit thymidine phosphorylase from Escherichia coli, human recombinant TP expressed in V79, and TP purified from human placenta. The IC(50) values ranged from 3.5 to 27μM.
3- 和 8-(8-膦酸辛基)-8-氮杂-7,9-二氮杂嘌呤，以及 1,8-双(8-氮杂-7,9-二氮杂嘌呤-8-基)辛烷被制备出来，并发现它们可以抑制来自大肠杆菌的胸苷磷酸化酶、在 V79 中表达的人重组 TP 以及从人胎盘纯化的 TP。IC(50)值范围为 3.5 至 27μM。
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