Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1254709 | Chinese Chemical Letters | 2014 | 4 Pages |
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.
Graphical abstractUsing a scaffold modification strategy, we identified a series of new 3-benzoheterocyclic substituted pyridopyrimidines as potential topoisomerase I inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide