Down, Kenneth published the artcileDiscovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode, Recommanded Product: 4-Amino-2-picoline, the publication is Journal of Medicinal Chemistry (2021), 64(18), 13780-13792, database is CAplus and MEDLINE.
Optimization of a previously reported lead series of PI3Kδ inhibitors with a novel binding mode led to the identification of a clin. candidate compound 31 (GSK251)(I). Removal of an embedded Ames-pos. heteroaromatic amine by reversing a sulfonamide followed by locating an interaction with Trp760 led to a highly selective compound 9 (II). Further optimization to avoid glutathione trapping, to enhance potency and selectivity, and to optimize an oral pharmacokinetic profile led to the discovery of compound 31 (GSK251) that had a low predicted daily dose (45 mg, b.i.d) and a rat toxicity profile suitable for further development.
Journal of Medicinal Chemistry published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Recommanded Product: 4-Amino-2-picoline.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem