Dual PTP1B/TC-PTP Inhibitors: Biological Evaluation of 3-(Hydroxymethyl)cinnoline-4()-Ones.

Dual inhibitors of protein phosphotyrosine phosphatase 1B (PTP1B)/T-cell protein phosphotyrosine phosphatase (TC-PTP) based on the 3-(hydroxymethyl)-4-oxo-1,4-dihydrocinnoline scaffold have been identified. Their dual affinity to both enzymes has been thoroughly corroborated by in silico modeling experiments. The compounds have been profiled in vivo for their effects on body weight and food intake in obese rats.

The carbene transfer to strong Lewis acids: copper is better than silver.

A new convenient approach to the synthesis of useful N-heterocyclic carbene complexes of group 13 metals was successfully developed. We demonstrate that air-stable copper(i) diaminocarbene complexes are excellent carbene transfer reagents for the synthesis of (IMes or IPr)MCl3 with high yields (M = Al, Ga). Use of this simple method allowed for the first time to obtain (IPr)AlCl3, inaccessible via a free carbene route.

Palladium(II)-Stabilized Pyridine-2-Diazotates: Synthesis, Structural Characterization, and Cytotoxicity Studies.

Well-defined diazotates are scarce. Here we report the synthesis of unprecedented homoleptic palladium(II) diazotate complexes. The palladium(II)-mediated nitrosylation of 2-aminopyridines with NaNO results in the formation of metal-stabilized diazotates, which were found to be cytotoxic to human ovarian cancer cells.