4,5,7-Trisubstituted indeno[1,2-b]indole inhibits CK2 activity in tumor cells equivalent to CX-4945 and shows strong anti-migratory effects.

Highly pleiotropic and constitutively active protein kinase CK2 is a key target in cancer therapy, but only one small-molecule inhibitor has reached clinical trials-CX-4945. In this study, we present the indeno[1,2-b]indole derivative 5-isopropyl-4-methoxy-7-methyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione (5a-2) that decreased the intracellular CK2 activity in A431, A549, and LNCaP tumor cell lines analogous to CX-4945 (> 75% inhibition at 20 µm) and similarly blocked CK2-specific Akt phosphorylation in LNCaP cells. Cellular uptake analysis demonstrated higher intracellular concentrations of 5a-2 (408.

Iodinated polymer nanoparticles as contrast agent for spectral photon counting computed tomography.

Suspensions of iodinated polymer nanoparticles are evaluated as contrast agent for Computed Tomography (CT) and Spectral Photon Counting Computed Tomography (SPCCT). Iodine containing moieties are grafted to poly(vinyl alcohol) by means of a covalent ester bond up to high degree of substitution of 0.77 providing high iodine content of 71 wt%.

QSAR Model of Indeno[1,2-]indole Derivatives and Identification of -isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3-]furan-3-carboxamide as a Potent CK2 Inhibitor.

Casein kinase II (CK2) is an intensively studied enzyme, involved in different diseases, cancer in particular. Different scaffolds were used to develop inhibitors of this enzyme. Here, we report on the synthesis and biological evaluation of twenty phenolic, ketonic, and -quinonic indeno[1,2-]indole derivatives as CK2 inhibitors.

Behaviour of Tetrabenazine in Acid Medium: Reassessment and Impact on Formulation.

Thorough studies of previous analytical stress data of tetrabenazine, a dopamine depleting agent, showed a potential susceptibility to acidic conditions. Hence, the behavior of tetrabenazine acidic solutions was studied by LC-MS and NMR spectroscopy. Reverse-phase LC-MS analysis of tetrabenazine acidic aqueous solutions consistently showed a main lipophilic impurity in a proportion of 15 to 20%.

Structure-based design and profiling of novel 17β-HSD14 inhibitors.

The human enzyme 17β-hydroxysteroid dehydrogenase 14 (17β-HSD14) oxidizes the hydroxyl group at position 17 of estradiol and 5-androstenediol using NAD as cofactor. However, the physiological role of the enzyme remains unclear. We recently described the first class of nonsteroidal inhibitors for this enzyme with compound 1 showing a high 17β-HSD14 inhibitory activity.