Repository logo

Infoscience

  • English
  • French
Log In
Logo EPFL, École polytechnique fédérale de Lausanne

Infoscience

  • English
  • French
Log In
  1. Home
  2. Academic and Research Output
  3. Journal articles
  4. Organometallic Ruthenium(II) Arene Compounds with Antiangiogenic Activity
 
research article

Organometallic Ruthenium(II) Arene Compounds with Antiangiogenic Activity

Nowak-Sliwinska, Patrycja  
•
Beijnum, Van
•
Judy, R.
Show more
2011
Journal of Medicinal Chemistry

The antimetastatic ruthenium (II) compounds [Ru(eta(6)-p-cymene)Cl-2(PTA)] (PTA = 1,3,5-triaza-7-phosphaadamantane) (RAPTA-C) and [Ru(eta(6)-toluene)Cl-2(PTA)] (RAPTA-T), as well as their analogues [Ru(eta(6)-p-cymene)Cl-2(DAPTA)] (DAPTA = (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo [3.3.1] nonane)) (DAPTA-C) and [Ru(eta(6)-toluene)Cl-2(DAPTA)] (DAPTA-T), respectively, were tested in in vitro bioassays for endothelial cell function. All compounds showed low toxicity profiles and similar dose-dependent antiproliferative effects in endothelial cells at 100 mu g/mL (similar to 200 mu M). EC migration, measured 6 h after drug exposure, was also efficiently inhibited (ED50 of similar to 300 mu g/mL, similar to 500 mu M, for all compounds). Since no cytostatic effect was noted, the inhibition of proliferation was considered mainly to consist of antiangiogenic activity. RAPTA-T and DAPTA-C were also tested in vivo in the chicken chorioallantoic membrane (CAM) assay and found to inhibit CAM development. Importantly, effective prevention of revascularization of the CAM after vaso-occlusive photodynamic therapy was observed. The reported ruthenium complexes show promising antimetastatic activity involving inhibition of angiogenesis and therefore are attractive agents for development of anticancer therapies based on combination of chemo- and angiostatic treatments.

  • Details
  • Metrics
Type
research article
DOI
10.1021/jm2002074
Web of Science ID

WOS:000291082500017

Author(s)
Nowak-Sliwinska, Patrycja  
Beijnum, Van
Judy, R.
Casini, Angela
Nazarov, Alexey A.
Wagnières, Georges  
van den Bergh, Hubert  
Dyson, Paul J.
Griffioen, Arjan W.
Date Issued

2011

Published in
Journal of Medicinal Chemistry
Volume

54

Issue

11

Start page

3895

End page

3902

Subjects

In-Vitro

•

Nami-A

•

Inhibits Angiogenesis

•

Photodynamic Therapy

•

Endothelial-Cells

•

Designed Peptide

•

Tumor-Growth

•

Rapta-C

•

Cancer

•

Complexes

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
GR-VDB  
Available on Infoscience
June 14, 2011
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/68701
Logo EPFL, École polytechnique fédérale de Lausanne
  • Contact
  • infoscience@epfl.ch

  • Follow us on Facebook
  • Follow us on Instagram
  • Follow us on LinkedIn
  • Follow us on X
  • Follow us on Youtube
AccessibilityLegal noticePrivacy policyCookie settingsEnd User AgreementGet helpFeedback

Infoscience is a service managed and provided by the Library and IT Services of EPFL. © EPFL, tous droits réservés