Cytotoxic RuII-p-cymene complexes of an anthraimidazoledione: halide dependent solution stability, reactivity and resistance to hypoxia deactivation

2019 ◽  
Vol 48 (21) ◽  
pp. 7187-7197 ◽  
Author(s):  
Amrita Sarkar ◽  
Sourav Acharya ◽  
Kumar Khushvant ◽  
Kallol Purkait ◽  
Arindam Mukherjee

Iodo coordinated half-sandwich RuII-anthraimidazoldione shows stability and low cytotoxicity even under hypoxia in metastatic cancer MDA-MB-231 cells (1–2 μM), induces apoptosis without ROS, and prevents migration at IC20 dose.

2017 ◽  
Vol 46 (13) ◽  
pp. 4382-4396 ◽  
Author(s):  
Orsolya Dömötör ◽  
Veronika F. S. Pape ◽  
Nóra V. May ◽  
Gergely Szakács ◽  
Éva A. Enyedy

Solution stability, chloride ion affinity and multidrug resistance selectivity of half-sandwich Rh(η5-C5Me5) and Ru(η6-p-cymene) complexes of 8-hydroxyquinolines.


2018 ◽  
Vol 42 (13) ◽  
pp. 11174-11184 ◽  
Author(s):  
János P. Mészáros ◽  
Orsolya Dömötör ◽  
Carmen M. Hackl ◽  
Alexander Roller ◽  
Bernhard K. Keppler ◽  
...  

Characterization, solution stability, chloride affinity and crystal structures of [Rh(η5-C5Me5)(N^N)(H2O)]2+ complexes and their correlation analysis.


2007 ◽  
Vol 20 (2) ◽  
pp. 213 ◽  
Author(s):  
Ji Yon Jo ◽  
Jeong Hoon Suh ◽  
Hwa Yong Shin ◽  
Yong Min Choi ◽  
Moon Sun Bang ◽  
...  

2020 ◽  
Author(s):  
Sofia Alexandra Milheiro ◽  
Joana Gonçalves ◽  
Ricardo Lopes ◽  
Margarida Madureira ◽  
Lis Lobo ◽  
...  

<p><a>A small library of “half-sandwich” cyclopentadienylruthenium(II) compounds of general formula [(</a>η<sup>5</sup>-C<sub>5</sub>R<sub>5</sub>)Ru(PPh<sub>3</sub>)(N-N)][PF<sub>6</sub>], a scaffold hitherto unfeatured in the toolbox of antiplasmodials, was screened for activity against the blood stage of CQ-sensitive 3D7-GFP, CQ-resistant Dd2 and artemisinin-resistant IPC5202 <i>Plasmodium falciparum</i> strains, and the liver stage of <i>P. berghei</i>. The best performing compounds displayed dual-stage activity, with single-digit nM IC<sub>50</sub> values against blood stage malaria parasites, nM activity against liver stage parasites, and residual cytotoxicity against mammalian cells (HepG2, Huh7). Parasitic absorption/distribution of 7-nitrobenzoxadiazole-appended fluorescent compounds <b>Ru4</b> and <b>Ru5</b> was investigated by confocal fluorescence microscopy, revealing parasite-selective absorption in infected erythrocytes and nuclear accumulation of both compounds. The lead compound <b>Ru2</b> impaired asexual parasite differentiation, exhibiting fast parasiticidal activity against both ring and trophozoite stages of a synchronized <i>P. falciparum</i> 3D7 strain. These results point to cyclopentadienylruthenium(II) complexes as a highly promising chemotype for the development of dual-stage antiplasmodials.</p>


2017 ◽  
Author(s):  
Christoph Engwer ◽  
Ronja Loy ◽  
Ioannis S. Chronakis ◽  
Ana C. Mendes ◽  
Francisco M. Goycoolea

Genipin is increasingly used as a crosslinking agent for chitosans due to its low cytotoxicity as a naturally occurring extract of the plant <i>Gardenia jasminoides</i>. Genipin reacts with the primary amino groups of chitosan to form blue hydrogels. We studied the gelation kinetics of different chitosans varying in their properties (molar mass 34 000-213 000 g mol<sup>-1</sup>, degree of acetylation 9-20%) and genipin in detail. We found that critical sol-gel transition times obtained from dynamic light scattering were in good agreement with the results obtained by small deformation oscillatory rheometry and microviscosimetry at high concentrations of chitosan. However, at below critical concentrations, we found a second regime of gelation that followed the same Ross-Murphy's gelation kinetics. The macroscopic appearance of these samples was a suspension of weak gel-like particles that were sensitive to mechanical forces. We believe that the material is a mesoscopic gel, as described for other polymers. To the best of our knowledge, this is the first time that this phenomenon has been described for the gelling system of chitosan and genipin.


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