A strategy for targeting protein kinases with large ATP-binding sites by using bulky and rigid octahedral ruthenium complexes as structural scaffolds is presented. A highly potent and selective GSK3 and Pim1 half-sandwich complex NP309 was successfully converted into a PAK1 inhibitor by making use of the large octahedral compounds Lambda-FL172 and Lambda-FL411 in which the cyclopentadienyl moie...

Ruthenium-catalyzed oxidative cyanation of tertiary amines with molecular oxygen in the presence of sodium cyanide and acetic acid gives the corresponding alpha-aminonitriles, which are highly useful intermediates for organic synthesis. The reaction is the first demonstration of direct sp(3) C-H bond activation alpha to nitrogen followed by carbon-carbon bond formation under aerobic oxidation c...

A new ruthenium(ii) polypyridyl-platinum(ii) diethynyl triad containing 3-ethynylphenanthroline linked by platinum(ii) bis-tributylphosphine organometallics, Ru(ii)-Pt(ii)-Ru(ii), and platinum(ii) bis-ethynylphenanthroline complex has been prepared. The ruthenium(ii)-metal triads, Ru(ii)-M-Ru(ii) (M = Pt(ii) and Au(i)), showed typical MLCT absorption bands and a lowest energy pi-pi* absorption ...

The phosphido complex RuCp*(PPh2CH=CHPPh2)(PPh2) (1) was exposed to a number of small molecules and was found to recognize and activate molecular oxygen in an unprecedented fashion: the ruthenium species split O2 in a ligand-based 4-electron reduction to produce an endo epoxide, as well as a phosphinito ligand. Based on XRD data, VT NMR studies, cyclooctene trapping studies, and crossover exper...

The slow dissociation of DNA threading intercalators makes them interesting as model compounds in the search for new DNA targeting drugs, as there appears to be a correlation between slow dissociation and biological activity. Thus, it would be of great value to understand the mechanisms controlling threading intercalation, and for this purpose we have investigated how the length of the bridging...

Two novel coordination compounds of half-sandwiched ruthenium(II) containing 2-(5-fluorouracil)-yl-N-(pyridyl)-acetamide were synthesized, and their intercalation binding modes with calf thymus DNA were revealed by hyperchromism of ultraviolet-visible spectroscopy; the binding constants were determined according to a Langmuir adsorption equation that was deduced on the base of careful cyclic vo...

A straightforward synthesis of substituted quinolines is described by cyclocondensation of anilines with 1,3-diols. The reaction proceeds in mesitylene solution with catalytic amounts of RuCl(3)·xH(2)O, PBu(3) and MgBr(2)·OEt(2). The transformation does not require any stoichiometric additives and only produces water and dihydrogen as byproducts. Anilines containing methyl, methoxy and chloro s...

Rhenium complex, [ReBr(CO)3(thf)]2-catalyzed reactions between aromatic imines and either acetylenes or α,β-unsaturated carbonyl compounds gave indene derivatives in good to excellent yields. These reactions proceed via C–H bond activation, insertion of acetylenes or α,β-unsaturated carbonyl compounds, intramolecular nucleophilic cyclization, and reductive elimination. Indene derivatives were a...

Tridentate amine-imine-phosphine ligands, R2PC5H7NC2H4NEt2 [(R)PNN(H)], where R = Pr(i) or Bu(t) are synthesized using a straightforward protocol of condensation, deprotonation, and addition of a chlorodialkylphosphine. Multinuclear NMR spectroscopy shows the ligands exist exclusively in the enamine tautomeric form in solution. Treating these ligands with RuHCl(PPr(i)3)2(CO) forms the desired c...

Angiogenesis is crucial for tumor growth. Thus, inhibiting angiogenesis represents a promising avenue for preventing tumor growth. This study investigated the anti-angiogenesis and anti-tumor effects of 8-hydroxyquinoline ruthenium(II) complexes [Ru(bpy)2(8-HQ)](+) (BQ) and [Ru(phen)2(8-HQ)](+) (PQ). The results showed that both compounds, especially PQ, suppressed the proliferation, migration,...