title: Dibenzo[c,h][1,5]naphthyridinediones as topoisomerase I inhibitors: design, synthesis, and biological evaluation.
abstract: Dibenzo[c,h][1,5]naphthyridinediones were prepared via a novel synthetic pathway. The compounds were designed as topoisomerase I (Top1) inhibitors based on the indenoisoquinoline series of drugs. The results of biological evaluation demonstrate that, unlike very closely related dibenzo[c,h][1,6]naphthyridinediones, dibenzo[c,h][1,5]naphthyridinediones retain the Top1 inhibitory activity of similarly substituted indenoisoquinolines.
authors.affiliation: Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy and The Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, United States.
authors.forename: Evgeny
authors.initials: E
authors.lastname: Kiselev
authors.forename: Nicholas
authors.initials: N
authors.lastname: Empey
authors.forename: Keli
authors.initials: K
authors.lastname: Agama
authors.forename: Yves
authors.initials: Y
authors.lastname: Pommier
authors.forename: Mark
authors.initials: M
authors.lastname: Cushman
mesh_terms: D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D004354:Drug Screening Assays, Antitumor; D007546:Isoquinolines / Q000737:chemistry*; D008958:Models, Molecular; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D007546:Isoquinolines; D009287:Naphthyridines; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I