- Pyridine methylamine compound and preparation method thereof
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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.
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Paragraph 0074-0080
(2021/08/28)
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- 2-SUBSTITUTED-6-BIARYLMETHYLAMINO-9-CYCLOPENTYL-9H-PURINE DERIVATIVES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS
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This invention relates to novel 2-substituted-6-biarylmethylamino-9-cyclopentyl-9H-purine derivatives, showing activity as specific inhibitors of growth and angiogenesis of hepatocellular carcinoma. The invention further includes pharmaceutical compositions containing the 2-substituted-6-biarylmethylamino-9-cyclopentylpurines.
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Paragraph 0089
(2016/03/08)
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- A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors
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The inhibition of overactive CDKs during cancer remains an important strategy in cancer drug development. We synthesized and screened a novel series of 2-substituted-6-biarylmethylamino-9-cyclopentylpurine derivatives for improved CDK inhibitory activity and antiproliferative effects. One of the most potent compounds, 6b, exhibited strong cytotoxicity in the human melanoma cell line G361 that correlated with robust CDK1 and CDK2 inhibition and caspase activation. In silico modeling of 6b in the active site of CDK2 revealed a high interaction energy, which we believe is due to the 6-heterobiarylmethylamino substitution of the purine moiety.
- Gucky, Tomá?,Jorda, Radek,Zatloukal, Marek,Bazgier, Václav,Berka, Karel,?ezní?ková, Eva,Béres, Tibor,Strnad, Miroslav,Kry?tof, Vladimír
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p. 6234 - 6247
(2013/09/02)
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- Synthesis, herbicidal activities, and 3D-QSAR of 2-cyanoacrylates containing aromatic methylamine moieties
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A series of novel 2-cyanoacrylates containing different aromatic rings were synthesized, and their structures were characterized by 1H NMR, elemental analysis, and single-crystal X-ray diffraction analysis. Their herbicidal activities against four weeds and inhibition of photosynthetic electron transport against isolated chloroplasts (the Hill reaction) were evaluated. Both in vivo and in vitro data showed that the compounds containing benzene, pyridine, and thiazole moieties gave higher activities than those containing pyrimidine, pyridazine, furan, and tetrahedronfuran moieties. To further explore the comprehensive structure-activity relationship on the basis of in vitro data, comparative molecular field analysis (CoMFA) was performed, and the results showed that a bulky and electronegative group around the para-position of the aromatic rings would have the potential for higher activity, which offered important structural insights into designing highly active compounds prior to the next synthesis.
- Liu, Yu-Xiu,Wei, Deng-Guo,Zhu, Ye-Rong,Liu, Shao-Hua,Zhang, Yong-Lin,Zhao, Qi-Qi,Cai, Bao-Li,Li, Yong-Hong,Song, Hai-Bin,Liu, Ying,Wang, Yong,Huang, Run-Qiu,Wang, Qing-Min
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experimental part
p. 204 - 212
(2009/04/11)
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