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Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer

De-Xuan Hu, Wen-Lin Tang, Yu Zhang, Hao Yang, Wenjie Wang, Keli Agama, Yves Pommier, Lin‐Kun An

2021Journal of Medicinal Chemistry28 citationsDOIOpen Access PDF

Abstract

showed an enhanced activity in drug-resistant MCF-7/TDP1 cancer cells and was synergistic with topotecan in both MCF-7 and MCF-7/TDP1 cells.

Topics & Concepts

TopoisomeraseChemistryCytotoxicityDNAPhosphodiesteraseEnzyme inhibitorCancer cellEnzymeDNA damageBiochemistryCancerIn vitroBiologyGeneticsCancer therapeutics and mechanismsNeutropenia and Cancer InfectionsAntibiotics Pharmacokinetics and Efficacy
Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer | Litcius