Abstract
2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine and a few of its 12-substituted analogs are active as TOP1-targeting agents. Studies were performed to further evaluate the potential of this series of non-camptothecin TOP1-targeting agents. The influence of a hydroxymethyl, formyl, N,N-dimethylaminomethyl, 2-(N,N-dimethylamino)ethyl, 3-(N,N-dimethylamino)propyl), and 4-(N,N-dimethylamino)butyl substituent at the 12-position on TOP1-targeting activity and tumor cell growth was evaluated. In addition, the relative pharmacologic activities of the 12-carboxamide analog, as well as its N-methyl and N,N-dimethyl derivatives were assessed.
| Original language | English |
|---|---|
| Pages (from-to) | 2877-2885 |
| Number of pages | 9 |
| Journal | Bioorganic and Medicinal Chemistry |
| Volume | 17 |
| Issue number | 7 |
| DOIs | |
| Publication status | Published - Apr 1 2009 |
| Externally published | Yes |
Keywords
- Benzo[i]phenanthridines
- Cytotoxicity
- Structure-activity
- Topoisomerase I
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry
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Feng, W., Satyanarayana, M., Tsai, Y. C., Liu, A. A., Liu, L. F., & LaVoie, E. J. (2009). 12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents. Bioorganic and Medicinal Chemistry, 17(7), 2877-2885. https://doi.org/10.1016/j.bmc.2009.02.023