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Discovery of a series of pyridopyrimidine derivatives as potential topoisomerase Ⅰ inhibitors 被引量:1
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作者 Jun-Peng Zhang Jie Huang +7 位作者 Chao Liu Xu-Fang Lu Bao-Xiang Wu Li Zhao Na Lu Qing-Long Guo Zhi-Yu Li Cheng Jiang 《Chinese Chemical Letters》 SCIE CAS CSCD 2014年第7期1025-1028,共4页
A series of new 3-benzoheterocyclic substituted pyridopyrimidines were designed and synthesized. Structures of the compounds were determined by IR, 1H NMR, and elemental analyses. The anti- proliferation activity of 1... A series of new 3-benzoheterocyclic substituted pyridopyrimidines were designed and synthesized. Structures of the compounds were determined by IR, 1H NMR, and elemental analyses. The anti- proliferation activity of 13 novel compounds was evaluated in A549, HL-60, BGC-823 and SMMC-7721 cell lines. Compounds 3, 5, 7, 8, 9,10 showed potent inhibitory activity against the four tested cancer cell lines. These six compounds were examined for Top I inhibition at 100 μmol/L by measuring the relaxation of supercoiled DNA in plasmid pBR322. Most of the tested compounds inhibited the enzyme at this concentration. The most potent compound 9 was as potent as camptothecin. 展开更多
关键词 Topoisomerase I inhibitors pyridopyrimidine ANTICANCER Synthesis
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