کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1254708 | 971387 | 2014 | 4 صفحه PDF | دانلود رایگان |
Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a–7d were synthesized and their antiproliferative activity against K562 and HepG-2 cell lines were evaluated. Compound 7c with pyridin-2-yl-methanamino group substituted at the C9 position of acridine showed good antitumor activity against both cell lines. The DNA-binding affinity of compound 7c was evaluated by UV–vis absorption spectra and fluorescence emission spectra. DNA topoisomerase I mediated relaxation of plasmid pBR322 DNA was also tested. Our results suggested that compound 7c with good antitumor activity and topoisomerase I inhibition activity can be developed as a prime candidate for further chemical optimization.
A series of acridine-based analogs 7a–7d were synthesized and tested for their antiproliferative activity against K562 and HepG-2 cancer cell lines, as well as DNA-binding properties. Compound 7c showed good antitumor activity and topoisomerase I inhibition activity, which makes it a good candidate for further chemical optimization.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 25, Issue 7, July 2014, Pages 1021–1024