Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.Safety of 1-Boc-4-(Aminomethyl)piperidine.
A series of 2,7-disubstituted thieno[3,2-d]pyrimidine derivatives I [R1 = 2-methoxy, 3-acetyl, 3-methylsulfonyl, etc.], II [R2 = methylcarbamoyl, piperidine-3-carbonylamino, diethoxyphosphorylmethyl, etc.], III [R3 = H, Me, ethoxy, etc.; R4 = H, fluoro, methyl; R5 = H, fluoro] and IV [R6 = pyrrolidin-3-yl, tetrahydro-2H-pyran-4-yl, piperidin-3-ylmethyl, etc.] were synthesized and evaluated as novel focal adhesion kinase (FAK) inhibitors. The novel 2,7-disubstituted thieno[3,2-d]pyrimidine scaffold was designed as a new kinase inhibitor platform that mimics the bioactive conformation of the well-known diaminopyrimidine motif. Most of the compounds potently suppressed the enzymic activities of FAK and potently inhibited the proliferation of U-87MG, A-549 and MDA-MB-231 cancer cell lines. Among these derivatives, the optimized compound III [R3 = R5 = H, R4 = fluoro] potently inhibited the enzyme (IC50 = 28.2 nM) and displayed stronger potency than TAE-226 in U-87MG, A-549 and MDA-MB-231 cells, with IC50 values of 0.16, 0.27, and 0.19μM, resp. Compound III [R3 = R5 = H, R4 = fluoro] also exhibited relatively less cytotoxicity (IC50 = 3.32μM) toward a normal human cell line, HK2. According to the flow cytometry results, compound III [R3 = R5 = H, R4 = fluoro] induced the apoptosis of MDA-MB-231 cells in a dose-dependent manner and effectively arrested MDA-MB-231 cells in G0/G1 phase. Further investigations revealed that compound III [R3 = R5 = H, R4 = fluoro] potently suppressed the migration of MDA-MB-231 cells. Collectively, these data support the further development of compound III [R3 = R5 = H, R4 = fluoro] as a lead compound for FAK-targeted anticancer drug discovery.
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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem