- 7-Amino-dibenzofuran-3-carboxylate: A new probe for femtosecond dynamic microsolvation studies of biomolecules
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The reorientational dynamics of a polar environment, for example water in the hydration shell of biomolecules, can be measured with a molecular probe by time-resolving its fluorescence Stokes shift. The new probe 7-amino- dibenzofuran-3-carboxylate (ADC)
- Berndt, Falko,Ioffe, Ilya,Granovsky, Alexander A.,Mahrwald, Rainer,Tannert, Sebastian,Kovalenko, Sergey A.,Ernsting, Nikolaus P.
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- Copper-Catalyzed One-Pot Synthesis of Dibenzofurans, Xanthenes, and Xanthones from Cyclic Diphenyl Iodoniums
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Oxygenation of cyclic diphenyl iodoniums (CDPIs) with varied medium-ring sizes has been fully investigated. This practical copper-catalyzed tandem reaction of CDPIs with water as the oxygen source enables the construction of derivatised dibenzofurans and xanthenes at moderate to good yields. Moreover, structurally important xanthones are also successfully accessed under the oxygenation conditions with additional TEMPO.
- Zhu, Daqian,Li, Min,Wu, Zhouming,Du, Yongliang,Luo, Bingling,Huang, Peng,Wen, Shijun
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supporting information
p. 4566 - 4571
(2019/07/09)
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- With Wnt signal path to inhibit the active heterocyclic compounds (by machine translation)
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The invention relates to a signal path with Wnt inhibiting activity of a heterocyclic compound, including the compound and its pharmaceutically acceptable salt, various isotope, various isomers or various crystal structure, having the general formula I of the structure shown in: the invention relates to a compound and its joint application composition can effectively inhibit the Wnt signal path, can be used for the treatment or prevention of a disorder associated with a Wnt signal path. (by machine translation)
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- Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’ amide scaffold
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The Wnt signaling pathway is an essential signal transduction pathway which leads to the regulation of cellular processes such as proliferation, differentiation and migration. Aberrant Wnt signaling is known to have an association with multiple cancers. Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Here we report the synthesis and structure–activity-relationship of the novel porcupine inhibitors based on a ‘reversed’ amide scaffold. The leading compound 53 was as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Compound 53 potently inhibited the secretion of Wnt3A, therefore was confirmed to be a porcupine inhibitor. Furthermore, compound 53 showed excellent chemical and plasma stabilities. However, the clearance of compound 53 in liver microsomal tests was moderate to high, and the solubility of compound 53 was suboptimal. Collective efforts toward further optimization of this novel tricyclic template to develop better porcupine inhibitors will be subsequently undertaken and reported in due course.
- Xu, Zhixiang,Xu, Xiangxiang,O'Laoi, Ruadhan,Ma, Haikuo,Zheng, Jiyue,Chen, Shuaishuai,Luo, Lusong,Hu, Zhilin,He, Sudan,Li, Jiajun,Zhang, Hongjian,Zhang, Xiaohu
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p. 5861 - 5872
(2016/10/30)
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- Synthesis of Dibenzofurans via C-H Activation of o-Iodo Diaryl Ethers
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An efficient method for the synthesis of dibenzofuran from o-iododiaryl ether using reusable Pd/C under ligand-free conditions has been developed. Synthesis of o-iododiaryl ether was achieved in one pot through sequential iodination and O-arylation of phenol under mild reaction conditions.
- Panda, Niranjan,Mattan, Irshad,Nayak, Dinesh Kumar
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p. 6590 - 6597
(2015/10/06)
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- TRICYCLIC COMPOUNDS AS MATRIX METALLOPROTEINASE INHIBITORS
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The present teachings relate to compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, R4, X, and Y are as defined herein. The present teachings also provide methods of making the compounds of formula I and methods of inhibiting matrix metalloproteinases, in particular, MMP-12, that may be involved in pathological disorders found in mammals, including a human.
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Page/Page column 74
(2010/09/17)
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- A Short Synthesis of Dibenzofurans and Dibenzothiophenes
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An afficient synthesis of dibenzofurans and dibenzothiophenes from aryl salicylates is described, which involves a novel rearrangement-extrusion-cyclisation sequence of o-substituted phenoxyl and thiophenoxyl radicals.
- Black, Michael,Cadogan, J. I. G.,McNab, Hamish
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p. 395 - 396
(2007/10/02)
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