[二脱氧尿苷]-[曲氟尿苷类似物]和[二脱氧胸苷]-[曲氟尿苷类似物]异二聚体作为HIV-1逆转录酶抑制剂的合成及抗HIV活性
Synthesis and anti-HIV activity of [d4U]-[trovirdine analogue] and [d4T]-[trovirdine analogue] heterodimers as inhibitors of HIV-1 reverse transcriptase.
作者信息
Gavriliu D, Fossey C, Ciurea A, Delbederi Z, Sugeac E, Ladurée D, Schmidt S, Laumond G, Aubertin A M
机构信息
Centre d'Etudes et de Recherche sur le Médicament de Normandie, U.F.R. des Sciences Pharmaceutiques, 5 Rue Vaubénard, 14032 Caen, France.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2002;21(8-9):505-33. doi: 10.1081/NCN-120015066.
A series of eleven heterodimers containing both a nucleoside analogue (d4U, d4T) and a non-nucleoside type inhibitor (Trovirdine analogue) were synthesized and evaluated for their ability to inhibit HIV replication. Unfortunately, the (N-3)d4U-Trovirdine conjugates (9a-e) and (N-3)d4T-Trovirdine conjugates (10a-f) were found to be inactive suggesting that the two individual inhibitor compounds do not bind simultaneously in their respective sites.
合成了一系列包含核苷类似物（d4U、d4T）和非核苷类抑制剂（曲韦林类似物）的11种异二聚体，并评估了它们抑制HIV复制的能力。遗憾的是，发现（N-3）d4U-曲韦林缀合物（9a-e）和（N-3）d4T-曲韦林缀合物（10a-f）无活性，这表明这两种单独的抑制剂化合物不会在各自的位点同时结合。
Zotero 插件