COA of Formula: C7H15NOIn 2013 ,《Structure-based discovery of cellular-active allosteric inhibitors of FAK》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Tomita, Naoki; Hayashi, Yoko; Suzuki, Shinkichi; Oomori, Yoshimasa; Aramaki, Yoshio; Matsushita, Yoshihiro; Iwatani, Misa; Iwata, Hidehisa; Okabe, Atsutoshi; Awazu, Yoshiko; Isono, Osamu; Skene, Robert J.; Hosfield, David J.; Miki, Hiroshi; Kawamoto, Tomohiro; Hori, Akira; Baba, Atsuo. The article conveys some information:
In order to develop potent and selective focal adhesion kinase (FAK) inhibitors, synthetic studies on pyrazolo[4,3-c][2,1]benzothiazines targeted for the FAK allosteric site were carried out. Based on the X-ray structural anal. of the co-crystal of the lead compound, 8-(4-ethylphenyl)-5-methyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazine 4,4-dioxide 1 with FAK, we designed and prepared 1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin derivatives which selectively inhibited kinase activity of FAK without affecting seven other kinases. The optimized compound, N-(4-tert-butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine 4,4-dioxide 30 possessed significant FAK kinase inhibitory activities both in cell-free (IC50 = 0.64 μM) and in cellular assays (IC50 = 7.1 μM). These results clearly demonstrated a potential of FAK allosteric inhibitors as antitumor agents. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4COA of Formula: C7H15NO)
2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKCOA of Formula: C7H15NO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem