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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, Spanien
  • 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, Spanien
  • 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, Spanien
  • 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, Spanien
  • 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, Spanien

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).

OriginalsprogEngelsk
TidsskriftEuropean Journal of Medicinal Chemistry
Vol/bind115
Sider (fra-til)179-190
Antal sider12
ISSN0223-5234
DOI
StatusUdgivet - 14 mar. 2016

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