156973-09-0Relevant articles and documents
Pyridine methylamine compound and preparation method thereof
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Paragraph 0125-0131, (2021/08/28)
The invention provides a pyridine methylamine compound and a preparation method thereof. The preparation method comprises the steps that tetrahydrofuran and sodium borohydride are sequentially added into a cyanopyridine compound, then an iodine-containing tetrahydrofuran solution is dropwise added, a reaction is conducted at the temperature of 20-30 DEG C, and after dropwise adding is completed, stirring is carried out continuously; after the reaction is finished, methanol is added for refluxing, extracting and spin-drying are carried out to obtain the pyridine methylamine compound; wherein a functional group in the cyanopyridine compound is selected from chlorine, bromine, methyl, ethyl, amino or hydrogen; according to the preparation method, high-temperature and high-pressure special equipment does not need to be used, so that the preparation method is relatively safe, and dangerous accidents such as explosion and fire disasters are avoided; besides, the preparation method is relatively environment-friendly, recycling treatment of hazardous waste (used Raney nickel) is not involved, the economic benefit is relatively high, borane generated by the synthesis method is converted into boric acid esters in the post-treatment process, the treatment cost is low, and the harm to the environment is much small.
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.
NOVEL QUINOLINE DERIVATIVES
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Page/Page column 121, (2008/06/13)
The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).