5,6-Dimethylxanthenone-4-acetic acid (DMXAA) and combretastatin A4 phosphate (CA-4-P) markedly inhibit tumor blood flow in mice and are both currently in clinical trial. One of the challenges in clinical evaluation of antivascular agents is the monitoring of tumor blood flow inhibition in individual patients. This study investigates, using mouse models, whether a new marker for tissue hypoxia, ...

UNLABELLED In vitro transendothelial permeability was compared to in vivo rat single-pass cerebral extractions to evaluate which method would best estimate the blood-brain barrier (BBB) permeability of several SPECT imaging agents. METHOD Six 99mTc complexes and seven non-Tc complexes were tested in vitro using monolayers of primary bovine brain microvessel endothelial cells and in vivo using...

The synthesis, kinetic, and spectral characterization of (7-nitrobenz-2-oxa-1,3-diazole)aminoethyl and (7nitrobenz-2-oxa1,3-diazole)aminopentyl methylphosphonofluoridate are described. These homologous organophosphorous agents contain the environmentally sensitive 7-nitrobenz-2-oxa1,3-diazole chromophore. They inhibit acetylcholinesterase from Torpedo at rates exceeding lo’ M” min” to form l...

Cell differentiation is essential for normal growth and homeostasis, and drug-induced differentiation of tumor cells into benign or normal cells is an important approach for anticancer chemotherapy. Studies of induction mechanisms for cell differentiation and discovery of differentiation-inducing factors are thus critical components of drug development. The Screening of differentiation-inducing...

The reaction of iron (II) with 2, 6-diacetylprydine dioxime (H2dapd) and 2-acetylprydine monoxime (Hapm) in 10% and 60% v/v ethanol-water solution at pH 2.5 and 7.5, respectively, were studied using direct and first derivative spectrophotometry. Fe (III) is reduced by H2dapd and gives iron (II) complex. A simple, rapid, selective and sensitive method for the determination of Fe (II), Fe (III) a...

Benzene, a ubiquitous human carcinogen, forms DNA adducts through its metabolites such as p-benzoquinone (p-BQ) and hydroquinone (HQ). N(2)-(4-Hydroxyphenyl)-2'-deoxyguanosine (N(2)-4-HOPh-dG) is the principal adduct identified in vivo by (32)P-postlabeling in cells or animals treated with p-BQ or HQ. To study its effect on repair specificity and replication fidelity, we recently synthesized de...

Arthrobacter protophormiae strain RKJ100 is capable of utilizing p-nitrophenol (PNP) as well as 4-nitrocatechol (NC) as the sole source of carbon, nitrogen and energy. The degradation of PNP and NC by this microorganism takes place through an oxidative route, as stoichiometry of nitrite molecules was observed when the strain was grown on PNP or NC as sole carbon and energy sources. The degradat...