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Influence of Hydrogen-Bonding Substituents on the Cytotoxicity of RAPTA Compounds

SCOLARO C
•
GELDBACH TJ
•
ROCHAT S
altro
DYSON PJ
2006
  • journal article

Periodico
ORGANOMETALLICS
Abstract
A new series of organometallic ruthenium(II)-arene compounds of the type RuCl2(è6-arene)(phosphine) (phosphine ) 1,3,5-triaza-7-phosphaadamantane, PTA, and 3,7-diacetly-1,3,7-triaza-5-phosphabicyclo- [3.3.1]nonane, DAPTA) with different potential hydrogen-bonding functionalities on the arene ligand have been prepared and studied for their antitumor activity. Cell viability studies using the TS/A mouse adenocarcinoma cancer cell line and the nontumorigenic HBL-100 human mammary cell line, combined with uptake determinations, are compared to the nonfunctionalized analogues, previously shown to be active on solid metastasizing tumors. The reactivity of the functionalized RAPTA compounds with a 14-mer oligonucleotide (established by mass spectrometry) has been rationalized by DFT calculations, which indicate that environmental factors are important.
WOS
WOS:000234906900026
Archivio
http://hdl.handle.net/11368/1701460
info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-33644547393
Diritti
metadata only access
Soggetti
  • Organometallic

  • Ruthenium

  • Drug

  • Tumour

  • Metabolism

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