Bandarage, Upul K.; Aronov, Alex M.; Cao, Jingrong; Come, Jon H.; Cottrell, Kevin M.; Davies, Robert J.; Giroux, Simon; Jacobs, Marc; Mahajan, Sudipta; Messersmith, David; Moody, Cameron S.; Swett, Rebecca; Xu, Jinwang published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors》.Electric Literature of C7H5N The article contains the following contents:
Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. PI3Kγ plays a critical role in mediating leukocyte chemotaxis as well as mast cell degranulation, making it a potentially interesting target for autoimmune and inflammatory diseases. We previously disclosed a novel series of PI3Kγ inhibitors derived from a benzothiazole core. The truncation of the benzothiazole core led to the discovery of a structurally diverse alkynyl thiazole series which displayed high PI3Kγ potency and subtype selectivity. Further medicinal chem. optimization of the alkynyl thiazole series led to identification of compounds such as 14 and 32, highly potent, subtype selective, and CNS penetrant PI3Kγ inhibitors. Compound 14 showed robust inhibition of PI3Kγ mediated neutrophil migration in vivo. In the part of experimental materials, we found many familiar compounds, such as 4-Ethynylpyridine(cas: 2510-22-7Electric Literature of C7H5N)
4-Ethynylpyridine(cas: 2510-22-7) belongs to pyridine. Pyridine is widely used in the precursor to agrochemicals and pharmaceuticals. Also, it is used as an important reagent and organic solvent.Electric Literature of C7H5N