DNA topoisomerases are essential enzymes that detangle chromosomes and modulate DNA supercoiling. Type II topoisomerases act by cleaving both strands of a DNA double helix and passing another double helix through the break. The catalytic cycle of the enzyme includes a transient “cleavage complex” in which the enzyme is covalently bound to the cleaved DNA ends. There are two types of topoisomerase II inhibitors; catalytic inhibitors (which inhibit the overall catalytic cycle of the enzyme) and poisons (which stabilize cleavage complexes). The majority of clinically used inhibitors, such as etoposide, doxorubicin, mitoxantrone and amsacrine are topoisomerase II poisons. A series of novel 9-amino acridones, differing in the functional group at C7 (compounds 1-3, with R = Br, Cl, and F, respectively) were synthesized. Furthermore, electron-withdrawing and electron-donating groups were also introduced on the 3-phenyl ring in order to establish structure-activity relationship (SAR). All compounds at 200 μM concentration were subsequently evaluated for topoisomerase II activity. The chloro-derivative was found to be more active in the above series, displaying DNA cleavage at 10 to 50 µM. The synthesis, characterization, and biochemical evaluation will be presented 

Novel 9-amino acridone derivatives as potential topoisomerase II inhibitors

Macromolecular Chemistry: The Second Century

[Author Benefits](https://scimeetings.acs.org/?utm_source=pubs_content_marketing&utm_medium=website&utm_campaign=0320_MCF_NPI_Launch_Spring_Homepage&ref=pubs_content_marketing)

[How to use SciMeetings](https://storage.googleapis.com/dl.morressier.com/acs/SciMeetings-ACSSpring2020-HowToGuide_M3020-Final.pdf)

[Frequently Asked Questions](https://storage.googleapis.com/dl.morressier.com/acs/SciMtng_ACSNMSp2020_FAQ_M3120_Final.pdf)

ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.