β-咔啉衍生物的合成与评价及其作为人类免疫缺陷病毒抑制剂的研究。
Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus.
机构信息
Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Punjab, India.
出版信息
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4416-9. doi: 10.1016/j.bmcl.2010.06.052. Epub 2010 Jun 12.
A series of beta-carboline derivatives were synthesized by utilizing aromatization and chemoselective alkylation method recently reported from our laboratory. Synthesized derivatives were evaluated for anti-HIV activity in human CD4+ T cell line (CEM-GFP) infected with HIV-1 NL(4.3) virus. 1-Formyl-beta-carboline-3-carbxylic acid methyl ester (15) showed inhibition of human immunodeficiency virus at IC(50)=2.9 microM.
最近，我们实验室利用芳香化和化学选择性烷基化方法合成了一系列β-咔啉衍生物。合成的衍生物在感染 HIV-1 NL(4.3)病毒的人 CD4+T 细胞系（CEM-GFP）中进行了抗 HIV 活性评估。1-甲酰基-β-咔啉-3-羧酸甲酯（15）在 IC(50)=2.9μM 时显示出对人类免疫缺陷病毒的抑制作用。
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