2539-53-9Relevant academic research and scientific papers
Coenzyme A-Conjugated Cinnamic Acids – Enzymatic Synthesis of a CoA-Ester Library and Application in Biocatalytic Cascades to Vanillin Derivatives
Dippe, Martin,Bauer, Anne-Katrin,Porzel, Andrea,Funke, Evelyn,Müller, Anna O.,Schmidt, Jürgen,Beier, Maria,Wessjohann, Ludger A.
supporting information, p. 5346 - 5350 (2019/11/29)
We present a bioorthogonal method for the ligation of coenzyme A (CoA) with cinnamic acids. The reaction, which is the initial step in the biosynthesis of a multitude of bioactive secondary metabolites, is catalyzed by a promiscuous plant ligase and yields CoA conjugates with different functionalization in high purity and without formation of by-products. Its applicability in biosynthetic cascades is shown for the direct transformation of cinnamic acids into natural benzaldehydes (like vanillin) or artificial derivatives (e. g. ethylvanillin). (Figure presented.).
Carbazole compound as Autotaxin inhibitor, preparation method therefor and application of carbazole compound
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Paragraph 0041; 0042, (2018/01/04)
The invention belongs to the technical field of biological pharmaceuticals and aims at providing a carbazole compound as an Autotaxin inhibitor, use of the compound in preparation of drugs for targeted inhibition of activity of the Autotaxin, use of the compound in preparation of drugs for treating and preventing diseases or symptoms caused by rising of lysophosphatidic acid and the Autotaxin, and use of the compound in preparation of antitumor drugs. The compound is a 2,7-substituted carbazole derivative, particularly 5-[7-(4-R2-benzyloxy)-9H-carbazol-2-methylene]-2-R1 phenol, R1-SWS-R2 for short, wherein R1 is methyl or ethyl, and R2 is any one of halogen, boric acid, sulfonyl, phospho, carboxyl and amino acid. The compound has very good anti-tumor activity to autocrine high-expression cell lines and has un-obvious influence on low-expression cell lines. The compound can be used for preparing corresponding antitumor drugs and provides possibility for designing novel Autotaxin inhibitors.
A 3, 4 - epoxy-cyclohexane METHYLAL glycol and its synthesis and use
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, (2017/11/16)
The invention discloses a 3,4-epoxy cyclohexyl methylal diol and a synthesis method thereof. The 3,4-epoxy cyclohexyl methylal diol can be used for synthesizing multiple vanillins and isovanillins. Compared with the existing synthesis process, the synthesis method disclosed by the invention has the advantages of simple steps and low discharge amount of three wastes.
A (3 - alkoxy - 4 - hydroxy) - cyclohexyl acetal glycol and its isomers of use
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, (2017/08/26)
The present invention discloses a (3-alkoxy-4-hydroxy)-cyclohexyl methylal diol, an (3-hydroxy-4-alkoxy)-cyclohexyl methylal diol and synthesis methods and use therefor. The (3-alkoxy-4-hydroxy)-cyclohexyl methylal diol and (3-hydroxy-4-alkoxy)-cyclohexyl methylal diol can be used for synthesis of a variety of vanillin and iso-vanillin. Compared to the existing synthetic method, the synthesis method has simple steps, and less discharge of "three wastes".
Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs
Zhao, Lei,Zhou, Jiu-Jiu,Huang, Xin-Ying,Cheng, Li-Ping,Pang, Wan,Kai, Zhen-Peng,Wu, Fan-Hong
, p. 993 - 999 (2015/08/19)
Abstract A total of 11 novel combretastatin A-4 (CA-4) analogs were designed, synthesized, and evaluated for the anti-proliferative effects in tumor cells. The compounds represent four structural classes: (i) hydrogenated derivatives, (ii) ethoxyl derivatives, (iii) amino derivatives and (iv) pro-drugs. Biological evaluations demonstrate that multiple structural features control the biological potency. Three of the compounds, sit-1, sit-2 and sit-3, have potent anti-proliferative activity against multiple cancer cell lines. Their pro-drugs were synthesized to increase water solubility. Structure-activity relationship study and Surflex-Docking were studied in this paper. These results will be useful for the design of new CA-4 analogs that are structurally related to the SAR study.
MONOCYCLIC PYRIDINE DERIVATIVE
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Paragraph 0406; 0407; 0408, (2014/09/03)
The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
ETHOXY DIPHENYL ETHANE DERIVATES, PREPARATION PROCESSES AND USES THEREOF
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, (2011/08/08)
The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4' position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3' thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3' to form amino acid amide water soluble prodrug having the structure shown as formula (I) the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.
PREPARATION AND THE USE OF ETHOXY COMBRETASTATINS AND THEIR PRODRUGS
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Page/Page column 7-8; fig.1, (2009/07/17)
The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4′-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3′-position of their B aryl ring. Similarly, 3′-amino combretastatin is 4′-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.
THE PREPARTION AND THE USE OF ETHOXY COMBRETASTATINS AND THEIR PRODRUGS
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Page/Page column 11; 19, (2009/06/27)
The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4'-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3'-position of their B aryl ring. Similarly, 3'-amino combretastatin is 4'-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.
BENZIMIDAZOLE DERIVATIVES AND MEDICAL USES THEREOF
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Page/Page column 35, (2008/06/13)
The present invention providesbenzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; R1 and R2 are H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; R3 is H, a halogen atom, optionally substituted alkyl group or the like; R9 and R5 are H, a halogen atom, OH or the like; and R6 and RX are H or OH: RY is F or OH.
