Chen, Lixue published the artcileThe synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC, Application In Synthesis of 39546-32-2, the publication is Bioorganic & Medicinal Chemistry (2018), 26(23-24), 6087-6095, database is CAplus and MEDLINE.
A series of 4-arylamido-2-arylaminoprimidines bearing acrylamide pharmacophore were synthesized as potent EGFRT790M/L858R inhibitors among which I [R1 = H, NR2R3 = N(CH2CH2)2CHCONH2] (IC50 = 0.5872 nM), I [R1 = H, NR2R3 = NMe2] (IC50 = 2.213 nM), or I [R1 = 3,4-(MeO)2, NR2R3 = N(CH2CH2)2NMe] (II) (IC50 = 12.57 nM) showed more potent anti-EGFRT790M/L858R activity compared with AZD-9291 (IC50 = 20.80 nM) and possessed high SI displaying 307.6, 56.5, or 12.5 for EGFRT790M/L858R over the wild-type resp. II also showed pretty good activity against H 1975 cells with an IC50 of 1.664 μM and exhibited low toxicity against the normal HBE cells (IC50 > 20 μM). II had moderate selectivity for H 1975 over A 431 (SI = 7.0) and the other selected cell lines. Morphol. staining results further indicated that II could promote apoptosis. Hence, II was a promising compound for further investigation as a potential EGFRT790M/L858R inhibitor for the treatment of NSCLC.
Bioorganic & Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Application In Synthesis of 39546-32-2.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem