6-芳基-2,4-二氧代-5-己烯酸，在基于细胞的检测中对HIV-1复制具有活性的新型整合酶抑制剂。
6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays.
作者信息
Costi Roberta, Di Santo Roberto, Artico Marino, Roux Alessandra, Ragno Rino, Massa Silvio, Tramontano Enzo, La Colla Massimiliano, Loddo Roberta, Marongiu M Elena, Pani Alessandra, La Colla Paolo
机构信息
Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università degli Studi di Roma 'La Sapienza', P. le A. Moro 5, I-00185 Rome, Italy.
出版信息
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1745-9. doi: 10.1016/j.bmcl.2004.01.037.
A series of 6-aryl-2,4-dioxo-5-hexenoic acids, were synthesized and tested against HIV-1 in cell-based assays and against recombinant HIV-1 integrase (rIN) in enzyme assays. Compound 8a showed potent antiretroviral activity (EC(50)=1.5 microM) and significant inhibition against rIN (strand transfer: IC(50)=7.9 microM; 3'-processing: IC(50)=7.0 microM). A preliminary molecular modeling study was carried out to compare the spatial conformation of 8a with those of L-731988 (4) and 5CITEP (7) in the IN core.
合成了一系列6-芳基-2,4-二氧代-5-己烯酸，并在基于细胞的试验中针对HIV-1以及在酶试验中针对重组HIV-1整合酶（rIN）进行了测试。化合物8a显示出有效的抗逆转录病毒活性（EC(50)=1.5微摩尔），并且对rIN有显著抑制作用（链转移：IC(50)=7.9微摩尔；3'-加工：IC(50)=7.0微摩尔）。进行了一项初步的分子建模研究，以比较8a与IN核心中L-731988（4）和5CITEP（7）的空间构象。
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