Wang, Ruifeng; Zhao, Xiangxin; Yu, Sijia; Chen, Yixuan; Cui, Hengxian; Wu, Tianxiao; Hao, Chenzhou; Zhao, Dongmei; Cheng, Maosheng published the artcile< Discovery of 7H-pyrrolo[2,3-d]pyridine derivatives as potent FAK inhibitors: Design, synthesis, biological evaluation and molecular docking study>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is pyrrolopyrimidine preparation antitumor docking focal adhesion kinase inhibitor SAR; 7H-pyrrolo[2,3-d]pyrimidine; Anticancer; Apoptosis; FAK inhibitor; Migration; Molecular docking.
Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy. Biol. evaluation indicated that most of these new compounds could potently inhibit FAK kinase, leading to the promising inhibitors against the proliferation of U-87MG, A-549, and MDA-MB-231 cancer cell lines. Among them, the optimized compound I potently inhibited the enzyme (IC50 = 19.1 nM) and displayed stronger potency than TAE-226 in U-87MG, A-549 and MDA-MB-231 cells, with IC50 values of 0.35, 0.24, and 0.34渭M, resp. Compound I is a multi-target kinase inhibitor. Furthermore, compound I also exhibited relatively less cytotoxicity (IC50 = 3.72渭M) toward a normal human cell line, HK2. According to the flow cytometry and wound healing assay results, compound I effectively induced apoptosis and G0/G1 phase arrest of MDA-MB-231 cells and suppressed the migration of U-87MG, A-549 and MDA-MB-231 cells. The docking study of compound I was performed to elucidate its possible binding modes and to provide a structural basis for the further structural guidance design of FAK inhibitors. Collectively, these data support the further development of compound I as a lead compound for FAK-targeted anticancer drug discovery.
Bioorganic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.
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