- A facile and versatile electro-reductive system for hydrodefunctionalization under ambient conditions
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A general electrochemical system for reductive hydrodefunctionalization is described, employing the inexpensive and easily available triethylamine (Et3N) as a sacrificial reductant. This protocol is characterized by facile operation, sustainable conditions, and exceptionally wide substrate scope covering the cleavage of C-halogen, N-S, N-C, O-S, O-C, C-C and C-N bonds. Notably, the selectivity and capability of reduction can be conveniently switched by simple incorporation or removal of an alcohol as a co-solvent.
- Huang, Binbin,Guo, Lin,Xia, Wujiong
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supporting information
p. 2095 - 2103
(2021/03/26)
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- NOVEL INHIBITORS OF HISTONE DEACETYLASE 10
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The present invention relates to novel inhibitors of histone deacetylase 10 (HDAC10), novel pharmaceutical compositions comprising such inhibitors, and to novel methods of treating diseases, such as cancer, autoimmune disorders or neurodegeneration, using such novel inhibitors or methods of using such novel inhibitors in organ transplantation.
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Paragraph 0167
(2020/10/18)
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- New 1,3-dioxolane and 1,3-dioxane derivatives as effective modulators to overcome multidrug resistance
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Multidrug resistance (MDR) to antitumor agents represents a major obstacle to a successful chemotherapy of cancer. Overexpression of P-glycoprotein (p-gp) seems to be the major factor responsible for MDR. A large number of chemically unrelated compounds are known to interact with p-gp resulting in a decreasing resistance. In our efforts related to structure-activity studies of new potential MDR reversal agents we synthesized a series of compounds that differ in the aromatic core structure, the linker, and the basic moiety. For our search of new aromatic core structures we synthesized novel 2,2-diphenyl-1,3-dioxolane, 2,2- diphenyl-1,3-dioxane, and 4,5-diphenyl-1,3-dioxolane derivatives. A range of lipophilic linker structures and protonable basic moieties were synthesized and investigated to optimize the structure of the potential MDR-modulators. The compounds were tested in vitro using human Caco-2 cells. Both the cytotoxicity of the synthons and their ability to resensitize the cells were determined with a MTT assay. The results show that at low concentration various substances reverse tumor cell MDR. Some of the new structures show better effects than established modulators like trifluoperazine.
- Schmidt, Matthias,Ungvari, Johannes,Gloede, Julia,Dobner, Bodo,Langner, Andreas
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p. 2283 - 2297
(2007/10/03)
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- Substituent Effect Studies of Aryl-Assisted Solvolyses. I. The Acetolysis of 2,2-Bis(substituted phenyl)ethyl p-Toluenesulfonates
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The substituent effect on the acetolysis of 2,2-bis(substituted phenyl)ethyl p-toluenesulfonates at 90.10 deg C can be described accurately in terms of the Yukawa-Tsuno (LArSR) relationship, giving a ρ value of -4.44 and an r value of 0.53. The substituent effect correlation of this system carrying two aryls is quite comparable to that of the 2-methyl-2-phenylpropyl system carrying a single aryl group, suggesting the close similarity in the structure of the transition states between the systems. The results can be reasonably accounted for on the basis of the accepted mechanism of this reaction, involving a rate-determining aryl-assisted transition state where only one aryl group of the two β-aryl groups participates.
- Fujio, Mizue,Maeda, Yasuyuki,Goto, Mutsuo,Saeki, Yoshihiro,Mishima, Masaaki,Tsuno, Yuho
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p. 3015 - 3020
(2007/10/02)
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