کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1254709 | 971387 | 2014 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery of a series of pyridopyrimidine derivatives as potential topoisomerase I inhibitors Discovery of a series of pyridopyrimidine derivatives as potential topoisomerase I inhibitors](/preview/png/1254709.png)
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.
Using a scaffold modification strategy, we identified a series of new 3-benzoheterocyclic substituted pyridopyrimidines as potential topoisomerase I inhibitors.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 25, Issue 7, July 2014, Pages 1025–1028