An article Cyclometalated Gold(III) Complexes Bearing DACH Ligands WOS:000475838000050 published article about GOLD-BASED DRUGS; CRYSTAL-STRUCTURE; ANTICANCER AGENTS; 2-SUBSTITUTED PYRIDINES; SOLUTION CHEMISTRY; CARBENE COMPLEXES; CYTOTOXICITY; REACTIVITY; DERIVATIVES; INHIBITION in [Gukathasan, Sailajah; Parkin, Sean; Awuah, Samuel G.] Univ Kentucky, Dept Chem, Lexington, KY 40506 USA in 2019.0, Cited 90.0. The Name is Phenyl(pyridin-2-yl)methanone. Through research, I have a further understanding and discovery of 91-02-1. Name: Phenyl(pyridin-2-yl)methanone
The synthesis of a novel class of cyclometalated gold(III) complexes supported by benzoylpyridine, benzylpyridine, and (1R,2R)-(+)-1,2-diaminocyclohexane (DACH) ligands, along with their crystal structures, is reported. These compounds provide a new scaffold to investigate biological properties of gold(III) complexes. The six complexes were prepared and characterized, following reactions of (C,N) cyclometalated gold(III) scaffolds, [Au(C boolean AND N)Cl-2] with DACH, which yielded a new series of cyclometaled gold(III), 3-5, of the type [Au(C boolean AND NH)(DACH)(2)](+) and the nitrogen substituted cyclometalated Au(III), 6-8, of the type [Au-(C boolean AND N)(DACH)](2+). Antiproliferative activity of these complexes in a panel of cancer cells showed promising results with IC50 in the micromolar range and selectivity over normal epithelial cells, MRCS. Whereas 8 shows minimal interaction with superhelical DNA except at high gold concentrations of 500 mu M, complex 5 does not show interaction even at 1000 mu M. The complexes display significant uptake in OVCAR8 cancer cells within 200-1200 pmol/million cells with the exception of complex 4. Differential cellular uptake was observed for the complexes; for example, while 3 and 8 display significant uptake, 4 showed minimal uptake. The compounds proved to be stable under physiological conditions and were minimally affected by either glutathione or sodium ascorbate. Cell cycle studies reveal a G1 arrest induced by representative complexes. The results reveal that enhanced Au(III) stabilization promoted by combined cyclometalated and DACH ligands may offer ligand tuning insights for novel anticancer drug design.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem