📜熊果酸置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 作为反应溶剂,以97 %的收率获得产物乌发醇 参考文献:Small Structural Differences Govern The Carbonic Anhydrase Ii Inhibition Activity Of Cytotoxic Triterpene Acetazolamide Conjugates 标题:Small Structural Differences Govern The Carbonic Anhydrase Ii Inhibition Activity Of Cytotoxic Triterpene Acetazolamide Conjugates 摘要:乙酰化三萜类化合物白桦脂素,齐墩果酸,熊果酸和甘草次酸被转化为琥珀酰-空位乙酰唑胺共轭物.利用几种人类肿瘤细胞系和非恶性成纤维细胞筛选了这些共轭物对碳酸酐酶 Ii 的抑制活性及其细胞毒性.结果表明,白桦脂酸和甘草次酸的抑制效果最好,而熊果酸和齐墩果酸的抑制效果明显较弱,但细胞毒性也较低.对人类 A375 黑色素瘤细胞而言,从白桦脂提取的共轭物的 Ki = 0.129 μm,Ec50 = 8.5 μm. DOI:10.3390/molecules28031009
专利号:US-10751419-B2 优先权日:2014-05-01 标题:Method for synthesis of reactive conjugate clusters 发明人:MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E 权利人:IONIS PHARMACEUTICALS INC 摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.
专利号:US-12146136-B2 优先权日:2020-03-26 标题:Synthesis of modified oligonucleotides with increased stability 发明人:KHVOROVA ANASTASIA; ROUX LOÃ?C MAURICE RENÉ JEAN; YAMADA KEN 权利人:UNIV MASSACHUSETTS 摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.
专利号:US-2012184724-A1 优先权日:2009-09-22 标 题 :Protected monomers and methods of deprotection for rna synthesis 发明人:SIERZCHALA AGNIESZKA B; SMART BRIAN PHILLIP; DELLINGER DOUGLAS J; DELLINGER GERALDINE; MYERSON JOEL; TIMAR ZOLTAN 权利人:SIERZCHALA AGNIESZKA B; SMART BRIAN PHILLIP; DELLINGER DOUGLAS J; DELLINGER GERALDINE; MYERSON JOEL; TIMAR ZOLTAN; AGILENT TECHNOLOGIES INC 摘要:A nucleoside monomer that is protected by a thionocarbamate protecting group and contains one or more 2 H, 13 C, or 15 N isotopes in the ribose and/or base part is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.
专利号:US-2019209694-A1 优先权日:2014-05-01 标 题 :Method for synthesis of reactive conjugate clusters
专利号:US-2024336916-A1 优先权日:2020-03-26 标 题:Synthesis of modified oligonucleotides with increased stability
专利号:US-8242258-B2 优先权日:2006-12-03 标题 :Protecting groups for RNA synthesis 发明人:DELLINGER DOUGLAS J; STELL BRIAN; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; STELL BRIAN; CARUTHERS MARVIN H; AGILENT TECHNOLOGIES INC; UNIV COLORADO 摘要:Aspects of the invention include 2′ protected nucleoside monomers that are protected at the 2′ site with orthoester-type protecting groups. The 2′ protected monomers also include a second, aryl carbonate-type, protecting group. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
1: Patrícia Gonçalves Tenório L, Xavier FHDC, Silveira Wagner M, Moreira Bagri K, Alves Ferreira EG, Galvani R, Mermelstein C, Bonomo AC, Savino W, Barreto E. Uvaol attenuates TGF-β1-induced epithelial-mesenchymal transition in human alveolar epithelial cells by modulating expression and membrane localization of β-catenin. Front Pharmacol. 2025 Jan 7;15:1504556. doi: 10.3389/fphar.2024.1504556. 2: Wang J, Liu W, Lu J, Zhu M, Wu Y, Pan W, Fan B, Song Y, Wang W, Chen G. Antineuroinflammatory Potential of Uvaol Transformation Products by Three Fungal Species. J Agric Food Chem. 2024 Dec 4;72(48):26762-26776. doi: 10.1021/acs.jafc.4c09088. Epub 2024 Nov 21. 13(8):578. doi: 10.3390/biology13080578. 5: Azzouni D, Alaoui Mrani S, Bertani R, Alanazi MM, En-Nabety G, Taleb M. Experimental and Theoretical Investigation of the Inhibitor Efficiency of Eucalyptus globulus Leaf Essential Oil (EuEO) on Mild Steel Corrosion in a Molar Hydrochloric Acid Medium. Molecules. 2024 Jul 15;29(14):3323. doi: 10.3390/molecules29143323.
合成参考文献
参考文献:10.3390/molecules16076010 摘要:Yang ZG, Matsuzaki K, Takamatsu S, Kitanaka S. Inhibitory effects of constituents from Morus alba var. multicaulis on differentiation of 3T3-L1 cells and nitric oxide production in RAW264.7 cells. Molecules. 2011 Jul 19;16(7):6010–22.