Abstract:
:A series of novel pyridyl acridone derivatives comprised of a pseudo-five-cyclic system to extend the π-conjugated acridone chromophore, were designed and synthesized as potent DNA binding antitumor compounds. Most synthesized compounds displayed good activity against human leukemia K562 cells in MTT tests, with compound 6d exhibiting the highest activity with IC50 value at 0.46 μM. Moreover, 6d showed potent activities against solid tumor cell lines (0.16-3.79 μM). Several experimental studies demonstrated that the antitumor mode of action of compound 6d involves DNA intercalation, topoisomerase I inhibition, and apoptosis induction through the mitochondrial pathway. In summary, compound 6d represents a novel and promising lead structure for the development of new potent anticancer DNA-binding agents.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Zhang B,Chen K,Wang N,Gao C,Sun Q,Li L,Chen Y,Tan C,Liu H,Jiang Ydoi
10.1016/j.ejmech.2015.02.003subject
Has Abstractpub_date
2015-03-26 00:00:00pages
214-26eissn
0223-5234issn
1768-3254pii
S0223-5234(15)00088-4journal_volume
93pub_type
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