Stereochemistry and 13C NMR spectra of some phenyl selenoethers obtained in phenylselenoetherification of olefinic alcohols

48-5

Simple synthesis of karahanaenone

1169-117

In vitro effects of some gold complexes on Na+/K+ ATPase activity and cell proliferation

The in vitro influence of gold(III) complexes, H[AuCl4], [Au(DMSO)(2)Cl-2]Cl and [Au(bipy)Cl-2]Cl (bipy = 2,2-bipyridine), upon commercially available Na+ /K+ ATPase activity, purified from porcine brain cortex, was investigated. Additionally, the complexes were tested on human lymphocytes, and incidence of micronuclei and cell proliferation index was determined. Concentration-dependent inhibition of the enzyme for all three compounds was obtained, but with differing potencies. Calculated IC50 from Hill analysis were (in M): 5.75 x 10(-7), 5.50 x 10(-6) and 3.98 x 10(-5), for H[AuCl4], [Au(DMSO)(2)Cl-2]Cl and [Au(bipy)Cl-2]Cl, respectively, while Hill coefficient values, n, were above 1 in all cases. This inhibition can be prevented using -SH donating ligands such as L-Cys and glutathione, and these ligands can also cause a recovery of the enzyme activity after the induced inhibition. Kinetic analysis demonstrated that each of the studied gold(III) complexes affects Na+ /K+ ATPase reducing maximum enzymatic velocity, V-max, but not significantly changing the affinity for the substrate (K-M value), implying a noncompetitive mode of the interaction. Furthermore, among investigated gold(III) complexes, the [Au(bipy)Cl-2]Cl complex exhibits a strong cytotoxic effect on human lymphocytes, which suggests its potential for use in antitumor therapy. (C(C) 2013 Elsevier Inc. All rights reserved

Organometallic half-sandwich iridium anticancer complexes

The low-spin 5d6 IrIII organometallic half-sandwich complexes [(η5-Cpx)Ir(XY)Cl]0/+, Cpx = Cp*, tetramethyl(phenyl)cyclopentadienyl (Cpxph), or tetramethyl(biphenyl)cyclopentadienyl (Cpxbiph), XY = 1,10-phenanthroline (4−6), 2,2′-bipyridine (7−9), ethylenediamine (10 and 11), or picolinate (12−14), hydrolyze rapidly. Complexes with N,N-chelating ligands readily form adducts with 9-ethylguanine but not 9-ethyladenine; picolinate complexes bind to both purines. Cytotoxic potency toward A2780 human ovarian cancer cells increases with phenyl substitution on Cp*: Cpxbiph > Cpxph > Cp*; Cpxbiph complexes 6 and 9 have submicromolar activity. Guanine residues are preferential binding sites for 4−6 on plasmid DNA. Hydrophobicity (log P), cell and nucleus accumulation of Ir correlate with cytotoxicity, 6 > 5 > 4; they distribute similarly within cells. The ability to displace DNA intercalator ethidium bromide from DNA correlates with cytotoxicity and viscosity of Ir−DNA adducts. The hydrophobicity and intercalative ability of Cpxph and Cpxbiph make a major contribution to the anticancer potency of their IrIII complexes

Isomer separation and gas-phase configurations of organoruthenium anticancer complexes : ion mobility mass spectrometry and modeling

We have used ion mobility-mass spectrometry combined with molecular modeling for the separation and configurational analysis of three low-molecular-weight isomeric organoruthenium anticancer complexes containing ortho-, meta-, or para-terphenyl arene ligands. The isomers were separated using ion mobility based on traveling-wave technology and the experimentally determined collision cross sections were compared to theoretical calculations. Excellent agreement was observed between the experimentally and theoretically derived measurements. (J Am Soc Mass Spectrom 2009, 20, 1119-1122) (C) 2009 American Society for Mass Spectrometr