[4-去氧尿苷]-丁炔-[HI-236]作为一种不可裂解的双功能核苷类逆转录酶抑制剂/非核苷类逆转录酶抑制剂用于抗HIV-1。
[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor.
作者信息
Hunter Roger, Muhanji Clare I, Hale Ian, Bailey Christopher M, Basavapathruni Aravind, Anderson Karen S
机构信息
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
出版信息
Bioorg Med Chem Lett. 2007 May 1;17(9):2614-7. doi: 10.1016/j.bmcl.2007.01.107. Epub 2007 Feb 4.
The synthesis of bifunctional compound 10 consisting of d4U joined at C-5 to a butynyl spacer attached to HI-236 is reported using a Sonogashira coupling as a key step. As a non-cleavable bifunctional HIV inhibitor incorporating an NRTI with an NNRTI, 10 shows good inhibitory activity (EC(50)=250 nM) against HIV (IIIB) replication in MT-2 cell culture, which is eight times greater than that of d4T and between those of the two component drugs.
报道了双功能化合物10的合成，该化合物由连接在C-5位的d4U与连接到HI-236的丁炔基间隔基组成，使用Sonogashira偶联作为关键步骤。作为一种包含核苷类逆转录酶抑制剂（NRTI）和非核苷类逆转录酶抑制剂（NNRTI）的不可裂解双功能HIV抑制剂，化合物10在MT-2细胞培养中对HIV（IIIB）复制显示出良好的抑制活性（EC(50)=250 nM），比d4T高8倍，且介于两种组分药物之间。
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