Fan, Yiqing; Zhang, Yongjie; Liu, Yan; Jiang, Hongyu; Zhou, Ying; Tang, Chunlei; Fan, Weizheng published the artcile< Pyrazolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: design, synthesis and biological evaluation>, Synthetic Route of 167938-56-9, the main research area is pyrazolopyrimidine macrocyclic preparation tropomyosin receptor kinase inhibition docking; Antitumor; Design and synthesis; High selectivity; The next-generation Trk inhibitor; Tropomyosin receptor kinase.
A series of pyrazolo[1,5-a]pyrimidine derivatives I [R = H, F, Cl; X1 = (CH2)2, CH2CMe2, (R)-CHMeCH2, (S)-CHMeCH2; X2 = (CH2)2, (CH2)3, (R)-CHMeCH2, (S)-CHMeCH2, (S)-CH2CHMe, (R)-CH2CHMe] was synthesized and evaluated the their biol. activity as the second-generation Trk inhibitors. The best compounds I [R = F; X1 = CH2CMe2; X2 = (R)-CHMeCH2] (IC50 = 1.40 and 1.80 nM, against TrkA, TrkAG595R, resp.) and I [R = F; X1 = (S)-CHMeCH2; X2 = (R)-CHMeCH2] (IC50 = 0.86, 6.92 nM, against TrkA, TrkAG595R, resp.) showed a kinase activity comparable to TPX-0005, and I [R = F; X1 = (S)-CHMeCH2; X2 = (R)-CHMeCH2] (IC50 = 350 nM against ALK) had a higher selectivity of Trk inhibition than TPX-0005, which was of great significance for reducing toxicity.
Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 167938-56-9 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H17NO3, Synthetic Route of 167938-56-9.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts