2539-53-9Relevant articles and documents
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.
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.