5896-29-7Relevant articles and documents
With Wnt signal path to inhibit the active heterocyclic compounds (by machine translation)
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Paragraph 0061-0063; 0068-0069, (2017/08/15)
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)
Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system
Xu, Zhixiang,Li, Jiajun,Wu, Yiyuan,Sun, Zhijian,Luo, Lusong,Hu, Zhilin,He, Sudan,Zheng, Jiyue,Zhang, Hongjian,Zhang, Xiaohu
, p. 154 - 165 (2015/12/04)
The Wnt signaling pathway is a critical developmental pathway which operates through control of cellular functions such as proliferation and differentiation. Aberrant Wnt signaling has been linked to the formation and metastasis of tumors. Porcupine, a member of the membrane-bound O-acyltransferase family of proteins, is an important component of the Wnt pathway. Porcupine catalyzes the palmitoylation of Wnt proteins, a process needed for their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from a known porcupine inhibitor class. The leading compound 59 demonstrated subnanomolar inhibition of Wnt signaling in a paracrine cellular assay. Compound 59 also showed excellent chemical, plasma and liver microsomal stabilities. Furthermore, compound 59 exhibited good pharmacokinetic profiles with 30% oral bioavailability in rat. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.
TRICYCLIC COMPOUNDS AS MATRIX METALLOPROTEINASE INHIBITORS
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Page/Page column 74, (2010/09/17)
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.
3-Nitrodibenzofuran and 3-Iododibenzofuran
Chaloner, Penny A.,Hitchcock, Peter B.,Sutton, Peter G.
, p. 2680 - 2683 (2007/10/02)
The structures of 3-nitrodibenzofuran, C12H7NO3, and 3-iododibenzofuran, C12H7IO, have been determined.Both molecules are nearly planar and pack in herringbone patterns composed of symmetry related head-to-tail pairs with parallel ? systems.
The Decomposition of Arenediazonium Tetrafluoroborates with Halo- and Azidotrimethylsilanes in Nonaqueous Solvents
Keumi, Takashi,Umeda, Toshiaki,Inoue, Yoshinori,Kitajima, Hidehiko
, p. 89 - 95 (2007/10/02)
The reaction of arenediazonium tetrafluoroborates with chlorotrimethylsilane in a tetrahydrofuran/N,N-dimethylformamide (DMF) (5v/3v) solution afforded the protodediazotization products in high yields.The reactions of the diazonium salts with halotrimethylsilanes in DMF were found to give the corresponding haloarenes.Among the halodediazotization reactions, the iododediazotization with iodotrimethylsilane proceeded smoothly at room temperature to give the iodoarenes in excellent yields.In a similar manner, a variety of azidoarenes were obtained in cosistently high yields by the treatment of arenediazonium tetrafluoroborates with azidotrimethylsilane in a DMF solution.
