Time filter

Source Type

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.

Loading Min Province Jointly Constructed Base For State Key Laboratory Shenzhen Key Laboratory Of Chemical Biology collaborators
Loading Min Province Jointly Constructed Base For State Key Laboratory Shenzhen Key Laboratory Of Chemical Biology collaborators