Design and Synthesis of Quinolizidine Derivatives as Influenza Virus and HIV-1 Inhibitors.
Design and Synthesis of Quinolizidine Derivatives as Influenza Virus and HIV-1 Inhibitors.
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DOI：
10.2174/0929867328666201229121802
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发表时间：
2021
影响因子：
4.1
通讯作者：
Chen CH
中科院分区：
文献类型：
--
作者：
Dang Z;Zhu L;Xie L;Lee KH;Malik F;Li Z;Huang L;Chen CH
我们以前曾报道过喹里西啶天然产物苦豆碱及其类似物在低μM浓度下可抑制流感病毒和/或HIV-1。本研究的目的是进一步优化苦豆碱以提高抗流感病毒活性。作为结构修饰的结果，苦豆碱衍生物可分为三个活性组：仅表现出抗HIV活性的那些、仅表现出抗流感病毒活性的那些、或针对两种病毒的活性的那些。针对有效抗流感活性优化的Aloperine通常失去抗HIV-1活性，反之亦然。化合物19以0.091 μM的IC 50抑制流感病毒PR 8复制，其效力分别比苦豆碱和先前报道的苦豆碱衍生物化合物3高约160倍和60倍。总之，数据表明苦豆碱是一种特殊的支架，可以被修饰成为一种特异性抗病毒化合物，对流感病毒或HIV-1的效力显著提高。
We have previously reported that a quinolizidine natural product, aloperine, and its analogs can inhibit influenza virus and/or HIV-1 at low μM concentrations. This study’s goal was to further optimize aloperine for improved anti–influenza virus activity. As a result of the structural modifications, aloperine derivatives can be classified into three activity groups: those that exhibit anti-HIV activity only, anti–influenza virus only, or activity against both viruses. Aloperine optimized for potent anti-influenza activity often lost anti-HIV-1 activity, and vice versa. Compound 19 inhibited influenza virus PR8 replication with an IC50 of 0.091 μM, which is approximately 160- and 60-fold more potent than aloperine and the previously reported aloperine derivative compound 3, respectively. In summary, the data suggest that aloperine is a privileged scaffold that can be modified to become a specific antiviral compound with markedly improved potency against influenza virus or HIV-1.
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影响因子：
4.2
作者：
Dang, Zhao;Xie, Hua;Chen, Chin-Ho
通讯作者：
Chen, Chin-Ho
Aloperine 通过双重细胞凋亡机制对多发性骨髓瘤发挥抗肿瘤作用。
影响因子：
28.5
作者：
Wang H;Yang S;Zhou H;Sun M;Du L;Wei M;Luo M;Huang J;Deng H;Feng Y;Huang J;Zhou Y
通讯作者：
Zhou Y
影响因子：
4.9
作者：
Lai, Weihong;Huang, Li;Chen, Chin-Ho
通讯作者：
Chen, Chin-Ho
DOI：
10.1080/21691401.2019.1699816
发表时间：
2020-01-01
影响因子：
5.8
作者：
Li, Weiwei;Li, Yanshu;Ren, Lina
通讯作者：
Ren, Lina
影响因子：
4.2
作者：
Dang, Zhao;Jung, Katherine;Chen, Chin-Ho
通讯作者：
Chen, Chin-Ho