RESUMO
Correction for 'Synthesis of glycerolipids containing simple linear acyl chains or aromatic rings and evaluation of their Mincle signaling activity' by Takanori Matsumaru et al., Chem. Commun., 2019, 55, 711-714, DOI: 10.1039/C8CC07322H.
RESUMO
Mincle, expressed in activated phagocytes, recognizes the lipid ligand to activate the innate immune system. We have synthesized glycerol derivatives possessing simple alkyl chains or aromatic rings and elucidated their structure-activity relationships using a Mincle-mediated signaling assay. The activity depends on the length of the simple acyl chains of the glycerol derivatives.
Assuntos
Lectinas Tipo C/metabolismo , Monoglicerídeos/farmacologia , Receptores Imunológicos/metabolismo , Transdução de Sinais/efeitos dos fármacos , Animais , Sítios de Ligação , Bovinos , Humanos , Lectinas Tipo C/química , Lectinas Tipo C/genética , Camundongos , Modelos Moleculares , Estrutura Molecular , Monoglicerídeos/síntese química , Monoglicerídeos/química , Mutação , Receptores Imunológicos/química , Receptores Imunológicos/genética , Relação Estrutura-Atividade , Linfócitos T/efeitos dos fármacosRESUMO
We accomplished divergent synthesis of potent kinase inhibitor BAY 61-3606 (1) and 27 derivatives via conjugation of imidazo[1,2-c]pyrimidine and indole ring compounds with aromatic (including pyridine) derivatives by means of palladium-catalyzed cross-coupling reaction. Spleen tyrosine kinase (Syk) and germinal center kinase (Gck, MAP4K2) inhibition assays showed that some of the synthesized compounds were selective Gck inhibitors.
