Small-molecule inhibitors of protein kinases have contributed immensely to our understanding of biological signaling pathways and have been exploited therapeutically for the treatment of cancers and other disease states. The pyridinyl imidazole compounds SB 203580 and SB 202190 were identified as ATP competitive antagonists of the p38 stress-activated protein kinases and have been widely used t...

Isocombretastatins are the not isomerizable 1,1-diarylethene isomers of combretastatins. Both families antimitotics poorly soluble and new analogs with improved water solubility needed. The ubiquitous 3,4,5-trimethoxyphenyl ring most its replacements contribute to problem. 39 compounds belonging two series isocombretastatin 2-chloro-6-methylsulfanyl-4-pyridinyl or 2,6-bis(methylsulfanyl)-4-pyri...

In the title compound, C(18)H(17)N(3)O(4), the furyl and phenyl rings are inclined at almost right angles [85.77 (7) and 63.25 (7)°, respectively] to the central imidazo[1,2-a]pyridinyl unit. The structure displays both inter- and intra-molecular N-H⋯O hydrogen bonding.

An air-stable dicationic Zn2+ complex (1) in a tripod-type ligand with non-bound phosphorus base and three pyridinyl “arms” (TPPh) was synthesized. Remarkably, while 2 mol% of 1 at room temperature selectively catalyzed dehydrogenative borylation terminal alkynes HBPin, lower loading (0.5 mol%) 90 °C promoted hydroboration reaction the same skipping step. The mode action proposed based on exper...

While investigating the role of p38 MAPK in regulating melanogenesis, we found that pyridinyl imidazole inhibitors class compounds as well as the analog compound SB202474, which does not inhibit p38 MAPK, suppressed both α-MSH-induced melanogenesis and spontaneous melanin synthesis. In this study, we demonstrated that the inhibitory activity of the pyridinyl imidazoles correlates with inhibitio...

The regulation in expression of human 5-hydroxytryptamine1A (5-HT1A) receptors by agonists and antagonists was studied in a stable transfected Chinese hamster ovary cell line expressing the human 5-HT1A receptor. Receptor density and affinity were measured with [125I]4-(2'-methoxyphenyl)-1-[2'-[N-(2'-pyridinyl)-p-iodobenzamido ]ethyl]piperazine ([125I]p-MPPI), a selective antagonist of 5-HT1A r...