97004-04-1Relevant articles and documents
Fabrication of ω-Transaminase@Metal-Organic Framework Biocomposites for Efficiently Synthesizing Benzylamines and Pyridylmethylamines
Chen, Lina,Ding, Yingying,Jiao, Qingcai,Liu, Junzhong,Yu, Jinhai,Zhang, Hongjuan,Zong, Weilu
, (2021/11/05)
In this study, ten ω-transaminases (ω-TAs) have been investigated to efficiently catalyze the synthesis of twenty-four functionalized benzylamines and pyridylmethylamines. We optimized the reactions, screened suitable amino donors and compared ω-transaminases activities for all aromatic aldehyde substrates. Under the optimized conditions, eighteen aromatic amines have been obtained with 60.4%–96.6% conversions and isolated only via simple extraction and recrystallization with 18.5%–81% yields on a preparative scale. Furthermore, we first immobilized the Bm-STA onto the MOFs via the physical adsorption to overcome the limitation of free enzyme and improve their industrial applications. The obtained Bm-STA/UiO-66-NH2 composites exhibited not only high enzymes loading (80.4 mg g?1) and enzyme activity recovery (95.8%), but also the better reusability, storage stability, pH stability and the tolerance to acetone and DMF.
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors
Dong, Guoqiang,Chen, Wei,Wang, Xia,Yang, Xinglin,Xu, Tianying,Wang, Pei,Zhang, Wannian,Rao, Yu,Miao, Chaoyu,Sheng, Chunquan
, p. 7965 - 7983 (2017/10/18)
Cancer metabolism and epigenetics are among the most intensely pursued research areas in anticancer drug discovery. Here we report the first small molecules that simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and histone deacetylase (HDAC), two important targets of cancer metabolism and epigenetics, respectively. Through iterative structure-based drug design, chemical synthesis, and biological assays, a highly potent dual NAMPT and HDAC inhibitor was successfully identified. Compound 35 possessed excellent and balanced activities against both NAMPT (IC50 = 31 nM) and HDAC1 (IC50 = 55 nM). It could effectively induce cell apoptosis and autophagy and ultimately led to cell death. Importantly, compound 35 showed excellent in vivo antitumor efficacy in the HCT116 xenograft model. This proof-of-concept study demonstrates the feasibility of discovering an inhibitor targeting cancer metabolism and epigenetics and provides an efficient strategy for multitarget antitumor drug discovery.
A N-(2 - (3 - (trifluoromethyl) phenoxy) - 4-pyridyl) a method for the synthesis of imines (by machine translation)
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Paragraph 0004; 0007, (2016/11/02)
This invention involves a kind of N-(2 the [...] (3 the [...] (trifluoromethyl) phenoxy) - 4 the [...] pyridyl) methylimine synthesis method, which belongs to the field of chemical synthesis. Traditional production N-(2 the [...] (3 the [...] (trifluoromethyl) phenoxy) - 4 the [...] pyridyl) methylimine process backwardness, long flow path, the yield is low, a large amount of the three wastes, it is difficult to control. The present invention provides a mild reaction conditions, the high yield of N-(2 the [...] (3 the [...] (trifluoromethyl) phenoxy) - 4 the [...] pyridyl) methylimine synthetic method. (by machine translation)