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Synthesis and biological evaluation of indeno[1,5]naphthyridines as topoisomerase I (TopI) inhibitors with antiproliferative activity

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  • Concepción Alonso, Departament de Química Orgánica I and Lascaray Research Center, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko Unibertsitatea, Paseo de la Universidad 7 Vitoria 01006, Spain
  • María Fuertes, Departament de Química Orgánica I and Lascaray Research Center, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko Unibertsitatea, Paseo de la Universidad 7 Vitoria 01006, Spain
  • María González, Departament de Química Orgánica I and Lascaray Research Center, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko Unibertsitatea, Paseo de la Universidad 7 Vitoria 01006, Spain
  • Gloria Rubiales, Departament de Química Orgánica I and Lascaray Research Center, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko Unibertsitatea, Paseo de la Universidad 7 Vitoria 01006, Spain
  • Cinzia Tesauro
  • Birgitta R Knudsen
  • Francisco Palacios, Departament de Química Orgánica I and Lascaray Research Center, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko Unibertsitatea, Paseo de la Universidad 7 Vitoria 01006, Spain

In an effort to establish new candidates with improved anticancer activity, we report here the synthesis of various series of 7H-indeno[2,1-c][1,5]-naphthyridines and novel 7H-indeno[2,1-c][1,5]-naphthyridine-7-ones and 7H-indeno[2,1-c][1,5]-naphthyridine-7-ols. Most of the products which were synthesized were able to inhibit Topoisomerase I activity. Moreover, in vitro testing demonstrated that a subset of the products exhibited a cytotoxic effect on cell lines derived from human breast cancer (BT 20), human lung adenocarcinoma (A 549), or human ovarian carcinoma (SKOV3).

Original languageEnglish
JournalEuropean Journal of Medicinal Chemistry
Volume115
Pages (from-to)179-190
Number of pages12
ISSN0223-5234
DOIs
Publication statusPublished - 14 Mar 2016

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