scholarly journals Synergetic anticancer activity of gold porphyrin appended to phenyl tin malonate organometallic complexes

2021 ◽  
Vol 50 (13) ◽  
pp. 4583-4592
Author(s):  
Christophe Nguyen ◽  
Isabelle Toubia ◽  
Stéphane Diring ◽  
Kamel Hadj-Kaddour ◽  
Magali Gary-Bobo ◽  
...  

The covalent attachment of these two anticancer chemotherapeutics makes it more efficient and selective than the equimolar mixture.

2013 ◽  
Vol 1 ◽  
Author(s):  
Muhammad Hanif ◽  
Samuel M. Meier ◽  
Alexey A. Nazarov ◽  
Julie Risse ◽  
Anton Legin ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 833
Author(s):  
Jahanzaib Arshad ◽  
Kelvin K. H. Tong ◽  
Sanam Movassaghi ◽  
Tilo Söhnel ◽  
Stephen M. F. Jamieson ◽  
...  

RuII(cym)Cl (cym = η6-p-cymene) complexes of pyridinecarbothioamides have shown potential for development as orally active anticancer metallodrugs, underlined by their high selectivity towards plectin as the molecular target. In order to investigate the impact of the metal center on the anticancer activity and their physicochemical properties, the Os(cym), Rh- and Ir(Cp*) (Cp* = pentamethylcyclopentadienyl) analogues of the most promising and orally active compound plecstatin 2 were prepared and characterized by spectroscopic techniques and X-ray diffraction analysis. Dissolution in aqueous medium results in quick ligand exchange reactions; however, over time no further changes in the 1H NMR spectra were observed. The Rh- and Ir(Cp*) complexes were investigated for their reactions with amino acids, and while they reacted with Cys, no reaction with His was observed. Studies on the in vitro anticancer activity identified the Ru derivatives as the most potent, independent of their halido leaving group, while the Rh derivative was more active than the Ir analogue. This demonstrates that the metal center has a significant impact on the anticancer activity of the compound class.


Metallodrugs ◽  
2015 ◽  
Vol 1 (1) ◽  
Author(s):  
Mario Kubanik ◽  
Jason K. Y. Tu ◽  
Tilo Söhnel ◽  
Michaela Hejl ◽  
Michael A. Jakupec ◽  
...  

Abstract3-Hydroxyflavones belong to the naturally occurring class of flavonoids and have been extensively studied with regard to medicinal application. Moreover, it has been demonstrated that these compounds act as bioactive chelates to the ruthenium(II)–arene moiety. Such organometallic complexes have shown promising anticancer activity against tumor cells via a multitargeting mode of action, interacting with DNA and inhibiting topoisomerase IIα. In this paper, we present the synthesis and characterization of an extended series of 3-hydroxyflavone ligands and their corresponding ruthenium-p-cymene complexes to study the impact of substitution pattern as well as of electron-withdrawing and –donating substituents at the flavonol-phenyl group. The ligands and complexes were characterized by elemental analysis, ESI-MS, 1D as well as 2D NMR spectroscopy. The structures of four Ru(η6-p-cymene) complexes were determined in solid state by single-crystal X-ray diffraction, and the impact of the substitution pattern with regard to in vitro anticancer activity in human cancer cell lines is discussed. Structural differences, calculated octanol-water partition coefficients (clogP) of the flavonols and aqueous solubility were used to rationalize the finding that chlorido[3-(oxo-κO)-2-(3,5- dimethoxyphenyl)-chromen-4-onato-κO](η6-p-cymene)ruthenium(II) 2b exhibits the highest cytotoxicity with IC50 values in the low μM range in all tested cell lines.


2007 ◽  
Vol 177 (4S) ◽  
pp. 294-294
Author(s):  
Nigel C. Phillips ◽  
Sonia Ménard ◽  
David S. Surprenant ◽  
Danbing Ke ◽  
Mario C. Filion

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
C Tamvakopoulos ◽  
ZD Sofianos ◽  
AL Skaltsounis ◽  
M Kritsanida

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
MA Zaki ◽  
V Samoylenko ◽  
S Khan ◽  
RM Abd slam ◽  
MH Hetta ◽  
...  

2014 ◽  
Vol 74 (S 01) ◽  
Author(s):  
JB Engel ◽  
S Meyer ◽  
J Dietl ◽  
B Kwok ◽  
O Ortmann ◽  
...  

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
S Sumkhemthong ◽  
M Suksomtip ◽  
P Chanvorachote ◽  
C Chaotham

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