Synthesis and anti-HIV activity of [ddN]-[ddN] dimers and benzimidazole nucleoside dimers.
In an attempt to combine the HIV-inhibitory capacity of different 2',3'-dideoxynucleoside (ddN) analogs, we have designed and synthesized several dimers of [AZT]-[AZT] and [AZT]-[d4T]. In addition, we also synthesized the dimers of 1-(1H-benzimidazol-1-yl)-1-deoxy-beta-D-ribofuranose. The in vitro anti-HIV activity of these compounds on a pseudotype virus, pNL4-3.Luc.R-E-, in the 293T cells has been determined. Among these compounds, 2,2'-(propane-1,3-diyl)bis[1-(beta-D-ribofuranosyl)-1H-benzimidazole] showed the highest anti-HIV activity with similar effect as AZT.
Li
Guo-Rui
GR
College of Chemistry and Molecular Sciences, Wuhan University, Hubei, Wuhan 430072, P. R. China.
Liu
Jun
J
Pan
Qin
Q
Song
Zhi-Bin
ZB
Luo
Feng-Ling
FL
Wang
Shao-Ru
SR
Zhang
Xiao-Lian
XL
Zhou
Xiang
X
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015224:Dideoxynucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D019281:Dimerization; D016655:HIV Core Protein p24 / Q000378:metabolism; D006801:Humans; D009705:Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015215:Zidovudine / Q000737:chemistry
C547372:2,2'-(propane-1,3-diyl)bis(1-(ribofuranosyl)-1H-benzimidazole); D019380:Anti-HIV Agents; D001562:Benzimidazoles; D015224:Dideoxynucleosides; D016655:HIV Core Protein p24; D009705:Nucleosides; D015215:Zidovudine; C031000:benzimidazole