Synthesis and Biological Evaluation of Nitrated 7-, 8-, 9-, and 10- Hydroxyindenoisoquinolines as Potential Dual Topoisomerase I (Top1)−Tyrosyl-DNA Phosphodiesterase I (TDP1) Inhibitors

The structure–activity relationships and hit-to-lead optimization of dual Top1–TDP1 inhibitors in the indenoisoquinoline drug class were investigated. A series of nitrated 7-, 8-, 9-, and 10-hydroxyindenoisoquinolines were synthesized and evaluated. Several compounds displayed potent dual Top1–TDP1...

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Publicado en:J Med Chem
Autores principales: Nguyen, Trung Xuan, Abdelmalak, Monica, Marchand, Christophe, Agama, Keli, Pommier, Yves, Cushman, Mark
Formato: Artigo
Lenguaje:Inglês
Publicado: 2015
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Article
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC7747014/
https://ncbi.nlm.nih.gov/pubmed/25811317
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b00136
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