4.7 Article

Near-infrared emitting fluorescent homobimetallic gold(I) complexes displaying promising in vitro and in vivo therapeutic properties

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 220, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113483

Keywords

Theranostics; NIR fluorescence; aza-BODIPY; Gold complexes; cancer; optical imaging

Funding

  1. Ministere de l'Enseignement Superieur et de la Recherche
  2. Center National de la Recherche Scientifique (CNRS)
  3. Conseil Regional de Bourgogne [2015-9205AAO033S04139/BG0003203, 2018Y-08158]
  4. Conseil Regional de Bourgogne Franche-Comte (France) [CRBFC 2020-Y-18612]
  5. French Research National Agency (ANR) [ANR-16-CE07-0020, ANR-18-CE18-0012]
  6. Universite de Bourgogne
  7. Conseil Regional de Bourgogne through the Plan d'Actions Regional pour l'Innovation (PARI)
  8. European Union through the PO FEDER-FSE Bourgogne 2014/2020 programs
  9. Ligue contre le Cancer, Comite de Cote d'Or
  10. Agence Nationale de la Recherche (ANR) [ANR-18-CE18-0012, ANR-16-CE07-0020] Funding Source: Agence Nationale de la Recherche (ANR)

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Three near-infrared optical theranostic systems based on homo-bimetallic gold(I)-aza-BODIPY complexes were synthesized, characterized, and studied in vitro and in vivo. These complexes showed trackable properties through near-infrared optical imaging and demonstrated anti-proliferative effects on human and murine cancer cell lines. The injection of the most promising agent resulted in significant anti-cancer activity in CT26 tumor-bearing mice.
Three near-infrared (NIR-I) optical theranostic systems were synthesized, characterized and studied in vitro and in vivo. These original homo-bimetallic gold(I)-based aza-BODIPY complexes proved to be trackable through near-infrared optical imaging in cells and in mice. They display anti-proliferative properties in micromolar range against human and murine cancer cell lines (4T1, MDA-MB-231, CT26, and SW480). Moreover, the injection of the most promising theranostic agent in CT26 tumor-bearing BALB/c mice induced a significant anti-cancer activity. (C) 2021 Elsevier Masson SAS. All rights reserved.

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