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Lang X.,Tsinghua University | Lang X.,Min Province Jointly Constructed Base For State Key Laboratory Shenzhen Key Laboratory Of Chemical Biology | Li L.,Min Province Jointly Constructed Base For State Key Laboratory Shenzhen Key Laboratory Of Chemical Biology | Chen Y.,Design Science | And 11 more authors.
Bioorganic and Medicinal Chemistry | Year: 2013

Acridine derivatives have been explored as DNA-binding anticancer agents. Some derivatives show undesired pharmacokinetic properties and new derivatives need to be explored. In this work, a series of novel acridine analogues were synthesized by modifying previously unexplored linkers between the acridine and benzene groups and their antiproliferative activity and the DNA-binding ability were evaluated. Among these derivatives, compound 5c demonstrated DNA-binding capability and topoisomerase I inhibitory activity. In K562 cell lines, 5c induced apoptosis through mitochondria-dependent intrinsic pathways. These data suggested that compound 5c and other acridine derivatives with modified linkers between the acridine and benzene groups might be potent DNA-binding agents. © 2013 Elsevier Ltd. All rights reserved. Source

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