Jiang Hong, Zhang Wen-Jin, Li Peng-Hui, Wang Jian, Dong Chang-Zhi, Zhang Kun, Chen Hui-Xiong, Du Zhi-Yun
Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China.
Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou 510006, China.
Bioorg Med Chem Lett. 2018 May 1;28(8):1320-1323. doi: 10.1016/j.bmcl.2018.03.017. Epub 2018 Mar 6.
In this study, a series of carbazole-rhodanine conjugates was synthesized and evaluated for their Topoisomerase II inhibition potency as well as cytotoxicity against a panel of four human cancer cell lines. Among these thirteen compounds, 3a, 3b, 3g, and 3h possessed Topoisomerase II inhibition potency at 20 μM. Mechanism study revealed that these compounds may function as Topo II catalytic inhibitors. It was found that the electron-withdrawing groups on the phenyl ring of compounds played an important role on enhancing both enzyme inhibition and cytotoxicity.
在本研究中，合成了一系列咔唑-罗丹宁共轭物，并评估了它们对拓扑异构酶II的抑制活性以及对四种人类癌细胞系的细胞毒性。在这13种化合物中，3a、3b、3g和3h在20μM时具有拓扑异构酶II抑制活性。机制研究表明，这些化合物可能作为拓扑异构酶II催化抑制剂发挥作用。发现化合物苯环上的吸电子基团在增强酶抑制和细胞毒性方面起着重要作用。
