Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitors
Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitors
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3-取代茚并异喹啉衍生物作为拓扑异构酶 I 抑制剂的设计、合成和生物学评价
DOI：
10.1016/j.bmcl.2015.12.014
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发表时间：
2016
影响因子：
2.7
通讯作者：
Zhiyu Li
中科院分区：
文献类型：
--
作者：
Qian Zhao;Xi Xu;Zhouling Xie;Xiao Liu;Qidong You;Qinglong Guo;Yi Zhong;Zhiyu Li
设计并合成了一系列新的茚并异喹啉衍生物。在HepG 2、A549和HCT-116细胞系中评价了这些新化合物的体外抗增殖活性。化合物9a、9 b、10a、10 c、10 e、18 a和18 b对三种测试的癌细胞系表现出有效的抑制活性。还检测了19种化合物在50 μM下对Top I的抑制作用。几乎所有测试化合物在该浓度下均显示出有效的Top I抑制活性。最有效的化合物9a和10a表现出比HCPT和TPT更大的细胞毒性，并且在我们的生物测定中在抑制Top I的活性方面与CPT相当。
A new series of indenoisoquinoline derivatives was designed and synthesized. The in vitro anti-proliferative activity of these novel compounds was evaluated in HepG2, A549 and HCT-116 cell lines. Compounds9a,9b,10a,10c,10e,18aand18bmanifested potent inhibitory activity against the three tested cancer cell lines. Nineteen compounds were also tested for Top I inhibition at 50 μM. Almost all the tested compounds showed potent Top I inhibition activity at this concentration. The most potent compounds9aand10ademonstrated more cytotoxicity than HCPT and TPT and was comparable to CPT in inhibitory activities on Top I in our biological assay.