Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y₆ receptor antagonists.

ABSTRACT: P2Y₆ receptor (P2Y₆R) antagonists represent potential drugs for treating cancer, pain, neurodegeneration, asthma, diabetes, colitis and other disorders. However, there are few chemical classes of known competitive antagonists. We recently explored the structure activity relationship (SAR) of 2H-chromene derivatives as P2Y₆R antagonists of moderate affinity. New analogues in this series modified at five positions were synthesized and shown to antagonize Ca²⁺ transients induced by the native agonist UDP in human (h) P2Y₆R-expressing (but not turkey P2Y₁R-, hP2Y₂R- or hP2Y₄R-expressing) astrocytoma cells. Alternatives to the reported 2-(trifluoromethyl)- and 3-nitro- substitutions of this scaffold were not

SUBMITTER: Jung YH 

PROVIDER: S-EPMC9555146 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature