2'-氟修饰的核苷膦酸酯的合成及其抗HIV活性：GS-9148类似物
Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148.
作者信息
Mackman Richard L, Lin Kuei-Ying, Boojamra Constantine G, Hui Hon, Douglas Janet, Grant Deborah, Petrakovsky Oleg, Prasad Vidya, Ray Adrian S, Cihlar Tomas
机构信息
Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1116-9. doi: 10.1016/j.bmcl.2007.11.126. Epub 2007 Dec 5.
Modified purine analogs of GS-9148 [5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid (2'-Fd4AP) were synthesized and their anti-HIV potency evaluated. The antiviral activity of guanosine analog (2'-Fd4GP) was comparable that of to 2'-Fd4AP in MT-2 cells, but selectivity was reduced.
合成了GS-9148 [5-(6-氨基嘌呤-9-基)-4-氟-2,5-二氢呋喃-2-基氧甲基]-膦酸（2'-Fd4AP）的修饰嘌呤类似物，并评估了它们的抗HIV效力。鸟苷类似物（2'-Fd4GP）在MT-2细胞中的抗病毒活性与2'-Fd4AP相当，但选择性降低。
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