178321-69-2Relevant academic research and scientific papers
Vinylboronic Acids as Efficient Bioorthogonal Reactants for Tetrazine Labeling in Living Cells
Eising, Selma,Van Der Linden, Nicole G. A.,Kleinpenning, Fleur,Bonger, Kimberly M.
, p. 982 - 986 (2018)
Bioorthogonal chemistry can be used for the selective modification of biomolecules without interfering with any other functionality present in the cell. The tetrazine ligation is very suitable as a bioorthogonal reaction because of its selectivity and hig
Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors
Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Minegishi, Hidemitsu,Ban, Hyun Seung,Nakamura, Hiroyuki
scheme or table, p. 1453 - 1456 (2010/07/06)
A series of boron-containing phenoxyacetanilide derivatives 8a-f, 9a-f, 15, and 16 were synthesized as hypoxia-inducible factor (HIF)-1α inhibitors. Among the compounds synthesized, carboranylphenoxyacetanilide 16 (GN26361) was found to be a potent inhibitor against HIF-1α accumulation under hypoxic conditions and inhibited the hypoxia-induced HIF-1 transcriptional activity in HeLa cells (IC50 = 0.74 μM). Compound 16 suppressed hypoxia-induced HIF-1α accumulation and vascular endothelial growth factor mRNA expression in a concentration-dependent manner without affecting the expression of HIF-1α mRNA.
Discovery of carboranes as inducers of 20S proteasome activity
Ban, Hyun Seung,Minegishi, Hidemitsu,Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Nakamura, Hiroyuki
experimental part, p. 1236 - 1241 (2011/02/21)
(Chemical Equation Presented) The carborane framework gives analogues able to induce 20S proteasome activities. A series of ortho-carboranylphenoxy derivatives were synthesized as 20S proteasome agonists, and carborane derivatives 11 a and 11 b were found
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA1/GPR40), a potential target for the treatment of type II diabetes
Christiansen, Elisabeth,Urban, Christian,Merten, Nicole,Liebscher, Kathrin,Karlsen, Kasper K.,Hamacher, Alexandra,Spinrath, Andreas,Bond, Andrew D.,Drewke, Christel,Ullrich, Susanne,Kassack, Matthias U.,Kostenis, Evi,Ulven, Trond
scheme or table, p. 7061 - 7064 (2009/11/30)
A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA1) has been discovered and explored. The preferred compound 20 (TUG-424, EC50 = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity.
Synthesis and luminescence of novel EuIII complexing agents and labels with 4-(phenylethynyl)pyridine subunits
Takalo, Harri,Hemmilae, Ilkka,Sutela, Timo,Latva, Martti
, p. 789 - 802 (2007/10/03)
The synthesis of novel 4-(phenylethynyl)pyridine subunits containing H2O-soluble complexing agents and their luminescence with EuIII ions are reported. Ligands with high luminescence intensities as well as quantum yields were obtained. Also the prepared labeling reagents as antibody conjugates gave the highest quantum and luminescence yields reported for H2O-soluble EuIII labels.
