Design, synthesis and biological evaluation of novel mansonone E derivatives prepared via CuAAC click chemistry as topoisomerase II inhibitors.
Design, synthesis and biological evaluation of novel mansonone E derivatives prepared via CuAAC click chemistry as topoisomerase II inhibitors.
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通过 CuAAC 点击化学制备的新型曼索酮 E 衍生物作为拓扑异构酶 II 抑制剂的设计、合成和生物学评价。
DOI：
10.1016/j.ejmech.2013.07.011
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发表时间：
2013
影响因子：
6.7
通讯作者：
Shi
中科院分区：
文献类型：
--
作者：
Zhi;Shi;Chun;Hua;Ding Li;Jia;Tian;Zhishu Huang;L. Gu;Shi
采用铜催化叠氮烯环加成点击化学的方法，合成了两个新的C-9氯和溴取代的C-3位含三氮唑基的曼松酮E衍生物。这些化合物被发现是拓扑异构酶II(Topo II)和拓扑异构酶I(Topo I)的有效抑制剂。Topo II介导的pBR322 DNA松弛和切割实验表明，这些衍生物可能是催化抑制剂。测定了它们对A549、HL-60、K562和HeLa细胞的细胞毒活性，表明这些化合物是一种有效的抗肿瘤药物。它们的构效关系和分子对接研究表明，三氮唑的取代基对细胞毒性特别重要。
Two series of novel C-9 chloro- and bromo-substituted mansonone E derivatives with triazole moieties at the C-3 position were prepared by using copper-catalysed azide–alkyne cycloaddition click chemistry. These compounds were found as potent inhibitors of topoisomerase II (Topo II) and topoisomerase I (Topo I). The Topo II-mediated pBR322 DNA relaxation and cleavage assay showed that the derivatives might act as catalytic inhibitors. Their cytotoxic activities against A549, HL-60, K562 and HeLa cells were evaluated, indicating that these compounds were potent antitumour agents. Their structure activity relationships and molecular docking study revealed that the substituents of the triazole were particularly important for cytotoxicity.
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beta-Lapachone 是一种新型 DNA 拓扑异构酶 I 抑制剂，其作用方式与喜树碱不同。
DOI：
--
发表时间：
1993
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Li,CJ;Averboukh,L;Pardee,AB
通讯作者：
Pardee,AB
影响因子：
11.2
作者：
Blanco E;Bey EA;Khemtong C;Yang SG;Setti-Guthi J;Chen H;Kessinger CW;Carnevale KA;Bornmann WG;Boothman DA;Gao J
通讯作者：
Gao J
β-拉帕酮和相关萘醌诱导 DNA 拓扑异构酶 II 介导的 DNA 切割。
影响因子：
11.2
作者：
Frydman,B;Marton,LJ;Sun,JS;Neder,K;Witiak,DT;Liu,AA;Wang,HM;Mao,Y;Wu,HY;Sanders,MM;Liu,LF
通讯作者：
Liu,LF
1,2-萘醌对人类肿瘤细胞生长的影响，且与其他抗癌药物缺乏交叉耐药性。
影响因子：
2.3
作者：
Dolan,ME;Frydman,B;Thompson,CB;Diamond,AM;Garbiras,BJ;Safa,AR;Beck,WT;Marton,LJ
通讯作者：
Marton,LJ
影响因子：
2.9
作者：
Fortune, JM;Velea, L;Osheroff, N
通讯作者：
Osheroff, N