Light-activated ruthenium polypyridyl anticancer prodrugs often suffer from poor water solubility, poor selectivity, and/or ill-defined intracellular targets. Coordination of the d- or l-glucose thioether ligand 3 (2-(2-(2-(methylthio)ethoxy)ethoxy)ethyl-β-glucopyranoside) to the highly lipophilic ruthenium complex [Ru(tpy)(dppn)(H2 O)]2+ ([1]2+ ; dppn=benzo[i]dipyrido-[3,2-a:2',3'-c]phenazine,...

Antibody-drug conjugates are targeted anticancer agents consisting of a cytotoxic drug covalently linked to a monoclonal antibody for tumor antigen-specific activity. Once bound to the target cell-surface antigen, the conjugate must be processed to release an active form of the drug, which can reach its intracellular target. Here, we used both biological and biochemical methods to better define...

Cytochrome c synthetase has been solubilized from yeast mitochondria using Triton X-100 and fractionated with ammonium sulfate. Use of this partially purified enzyme has permitted us to isolate a quantity of iso-1-cytochrome c formed from 125I-labeled apocytochrome c and hemin in the presence of a NADPH-generating system. Visible absorption spectra (pH 8.0 or 5.0) including alpha, beta, and Sor...

The reactions of 2-(mercaptoethyl)benzimidazole with 2-vinylpyridine and 2-picolyl chloride (in basic medium) yield the new unsymmetrical ligands 1-(2-benzimidazolyl)-5-(2 -pyridyl)-3-thiapentane (Biptp) and 1-(2-benzimidazolyl)-4-(2 -pyridyl)-3-thiabutane (Biptb), respectively. Copper(II) complexes of these ligands with differing anions were prepared. Crystal structures are reported for [Cu(Bi...

Surface-enhanced Raman scattering (SERS) spectra of methionine (Met) containing dipeptides: Met-X and X-Met, where X is: L-glycine (Gly), L-leucine (Leu), L-proline (Pro), and L-phenylalanine (Phe) are reported. Using pre-aggregated Ag colloid we obtained high-quality SERS spectra of these compounds spontaneously adsorbed on colloidal silver. Additionally, we measured Raman spectra (RS) of thes...

The influence of tridentate, nitrogen donor ligands, on the stability of gold(III) complexes under physiological conditions was investigated. The interaction of [Au(terpy)Cl](2+) (terpy = 2,2':6'2'' terpyridine), [Au(bpma)Cl](2+) (bpma = bis(pyridyl-methyl)amine), [Au(dien)Cl](2+) (dien = diethylenetriamine) and [AuCl4](-) with the biologically relevant thiols, L-cysteine (L-Cys) and glutathion...

The internalizing anti-Le(y) monoclonal antibody (MAb) BR64 was conjugated to the anticancer drug doxorubicin (DOX) using an acid-labile hydrazone bond to the DOX and either a disulfide or thioether bond to the MAb. The resulting disulfide (BR64-SS-DOX) and thioether (BR64-S-DOX) conjugates were evaluated for stability, potency, and antigen-specific activity in both in vitro and in vivo model s...