The present paper examines one of the multiple uses of the CellScan technique, its utilization in the biological evaluation of novel compounds, in order to improve the methods concerning the prediction of their anti-proliferative effects and application as anti-cancer drugs. The CellScan is a laser scanning static cytometer, enabling repetitive spectroscopic measurements in intact living cells. The detection of cell viability and apoptosis is possible, based on the transformations that occur in the cytoplasm matrix of tumour cells influenced by cytotoxic compounds. The measurement of fluorescence changes, due to this phenomenon, is possible with the CellScan system. The potential of this technology to detect the in vitro effects of the inhibitory molecules on tumour cells was demonstrated, making this method a valuable tool for chemosensitivity tests. We synthesized and fully characterised three novel platinum complexes of tertiary arsine ligands: trans-[PtI2(2-iPrOC6H4AsPh2)2] (), trans-[PtCl2(2-MeOC6H4AsPh2)2] () and cis-[PtCl2(2-HOC6H4AsPh2)2] (). The three compounds are biologically active against tumour cells and their cytotoxicity is comparable with standard drugs. Measurements using the CellScan technology correlate well with the results provided by other bioassay methods.
The structures of two 1 : 2 adducts between tin(IV) halides and AsPh(3) have been determined. SnCl(4)(AsPh(3))(2) adopts a six-coordinate geometry at tin in which the two organoarsine donors are mutually trans. In contrast, SnBr(4)(AsPh(3))(2) is five-coordinate at tin and only one arsine is directly bonded to the metal, in an axial site of the trigonal bipyramid. The second AsPh(3) group has a close contact with the axially bound bromine [As...Br: 3.567(3) angstroms], which is a unique structural variation that depicts an intermediate in a halogen-transfer reaction between Group 14 and Group 15 elements. AACVD using SnCl(4)(AsPh(3))(2) generates a film containing SnO(2) and a second crystalline material which is possibly SnCl(2), but which contains no arsenic.
The synthesis and characterization of 10-(o-alkoxyphenyl)phenoxarsines 2-ROC6H4As(C6H4)2O (R = H, Me, and Pri, As(C6H4)2O = phenoxarsine) and their platinum(II) and palladium(II) complexes cis-[PtCl2{2-PriOC6H4As(C6H4)2O-kappaAs}2] (1), trans-[PdCl2{2-PriOC6H4As(C6H4)2O-kappaAs}2] (2), cis-[PtCl2{2-HOC6H4As(C6H4)2O-kappaAs}2] (3), cis-[PdCl2{2-HOC6H4As(C6H4)2O-kappaAs}2] (4), cis-[PtI2{2-MeOC6H4As(C6H4)2O-kappaAs}2] (5), and trans-[PdCl2{2-MeOC6H4As(C6H4)2O-kappaAs}2] (6) are reported. The chelate complex cis-[Pt{2-OC6H4As(C6H4)2O-kappaAs,O}2] (7) is also described. The molecular structures of 1-4 and 7 were determined. The short As...O intramolecular interaction found in complexes 1-4 in the solid state was also verified by calculations at the B3LYP/LANL2DZ level for complex 2 and for 10-(o-isopropoxyphenyl)phenoxarsine in the gas phase, and this suggests that the interaction is a characteristic of the ligand rather than a packing effect. Calculations at the B3LYP/LANL2DZ and Oniom(B3LYP/LANL2DZ:uff) levels for complexes 1-4 showed that the solvent plays a crucial role in the crystallization (through geometry constraints) of the kinetically stable cis isomers.
An effective methodology has been developed for the synthesis of enantiopure 2,2′-dialkynylated 1,1′-binaphthalene derivatives. Enantiopure 2,2′-diiodo-1,1′-binaphthalene (10) provided 2,2′-diethynyl-1,1′-binaphthalene (16) in the Negishi alkynylation supported by microwave irradiation in a very good yield with conservation of stereochemical information. The Stephen-Castro alkynylation of 10 afforded products in lower yields; however, in stereoconservative manner as well. Terminal diacetylene 16 served as precursor in the Sonogashira cross-coupling reaction to give new bispyridine derivatives 7-9 as potential ligands in moderate to high yields. Coordination of bispyridines with Zn 2+ and Ag + ions was observed by NMR and CD spectroscopy. The coordination ability of bis(2-pyridylethynyl) derivative 7 to palladium cation was determined by X-ray structure analysis. Keywords: Sonogashira reaction; Alkynylations; Bispyridines; Binaphthalenes; C 2 -Symmetric ligands; Cross-coupling reactions; Palladium; Alkynes; Helicenes; Biaryls.Axial chirality as a unique stereochemical property of axially chiral 1,1′-binaphthalene derivatives substituted at the position 2 and 2′ plays a crucial role in their broad application in stereoselective synthesis 1 , in materials science 2 , in the separation and recognition of chiral compounds 3 . Substitution reactions, in particular cross-coupling reactions, at both positions 2 and 2′ are critical for conservation of stereochemical information in the course of preparation of such derivatives [4][5][6][7] . Specialty of the cross-coupling reactions (or any substitutions) at the positions 2 and 2′ consist in substan-
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