Li, Jianheng published the artcileDesign, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFRL858R/T790M inhibitors, Application In Synthesis of 505-10-2, the main research area is cyclopropylindolyl anilinopyrimidine preparation EGFR inhibitor structure activity; pyrimidine antitumor EGFR inhibition SAR docking apoptosis induction pharmacokinetic; Anti-proliferation; Anti-tumor efficacy in vivo; Epidermal growth factor receptor; L858R/T790M double mutants; Non-small cell lung cancer (NSCLC).
A new series of 2,4-diarylpyrimidine derivatives containing a cyclopropyl moiety, I [R = N(Me)(CH2)2OH, thiomorpholino, O(CH2)3SMe, etc., X = H; R = S(CH2)2NMe2, S(O)(CH2)2NMe2, X = Cl], were designed, synthesized and evaluated as novel selective EGFRL858R/T790M inhibitors. The most promising compound, I [R = S(:O)CH2CH2NMe2] (II), demonstrated excellent kinase inhibitory activity against EGFR double mutation with IC50 value of 0.26 nM. Moreover, II provided strong activity against H1975 cells with IC50 value of 0.008μM and exhibited little toxicity toward four non-tumorigenic cell lines. Furthermore, II showed potent antitumor efficacy in a murine EGFRL858R/T790M-driven H1975 xenograft model. These results indicated that II may be a promising drug candidate for further study.
European Journal of Medicinal Chemistry published new progress about Aminopyrimidines Role: ADV (Adverse Effect, Including Toxicity), PAC (Pharmacological Activity), PKT (Pharmacokinetics), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 505-10-2 belongs to class alcohols-buliding-blocks, name is 3-(Methylthio)propan-1-ol, and the molecular formula is C4H10OS, Application In Synthesis of 505-10-2.
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