Structure-activity relationship of novel acridone derivatives as antiproliferative agents

[Display omitted] Unlike other DNA topoisomerase II (topo II) inhibitors, our recently identified acridone derivative E17 exerted strong cytotoxic activity by inhibiting topo II without causing topo II degradation and DNA damage, which promoted us to explore more analogues of E17 by expanding its ch...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2021-01, Vol.29, p.115868-115868, Article 115868
Main Authors: Chen, Ji-Ning, Wu, Xing-Kang, Lu, Chun-Hua, Li, Xun
Format: Article
Language:English
Subjects:
Acridone derivatives
Antiproliferative efficacy
E17
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Summary:[Display omitted] Unlike other DNA topoisomerase II (topo II) inhibitors, our recently identified acridone derivative E17 exerted strong cytotoxic activity by inhibiting topo II without causing topo II degradation and DNA damage, which promoted us to explore more analogues of E17 by expanding its chemical diversification and enrich the structure–activity relationship (SAR) outcomes of acridone-oriented chemotypes. To achieve this goal, 42 novel acridone derivatives were synthesized and evaluated for their antiproliferative efficacies. SAR investigations revealed that orientation and spatial topology of R3 substituents make greater contributions to the bioactivity, exemplified by compounds E24, E25 and E27, which has provided valuable information for guiding further development of acridone derivatives as promising drug candidates.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2020.115868