Li, Bo; Li, Yongliang; Tomkiewicz-Raulet, Celine; Dao, Pascal; Lietha, Daniel; Yen-Pon, Expedite; Du, Zhiyun; Coumoul, Xavier; Garbay, Christiane; Etheve-Quelquejeu, Melanie; Chen, Huixiong published the artcile< Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma>, Related Products of 112-63-0, the main research area is malignant glioblastoma FAK cell migration cell cycle autophosphorylation.
Human malignant glioblastoma (GBM) is a highly invasive and lethal brain tumor. Targeting of integrin downstream signaling mediators in GBM such as focal adhesion kinase (FAK) seems reasonable and recently demonstrated promising results in early clin. studies. Herein, we report the structure-guided development of a series of covalent inhibitors of FAK. These new compounds displayed highly potent inhibitory potency against FAK enzymic activity with IC50 values in the nanomolar range. Several inhibitors retarded tumor cell growth as assessed by a cell viability assay in multiple human glioblastoma cell lines. They also significantly reduced the rate of U-87 cell migration and delayed the cell cycle progression by stopping cells in the G2/M phase. Furthermore, these inhibitors showed a potent decrease of autophosphorylation of FAK in glioblastoma cells and its downstream effectors Akt and Erk as well as nuclear factor-κB. These data demonstrated that these inhibitors may have the potential to offer a promising new targeted therapy for human glioblastomas.
Journal of Medicinal Chemistry published new progress about Cell cycle checkpoint (cell cycle arrest, at G2/M phase). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Related Products of 112-63-0.
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