90794-33-5Relevant 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 (2018/04/23)
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
Synthesis and biological evaluation of ortho-carborane containing benzoxazole as an inhibitor of hypoxia inducible factor (HIF)-1 transcriptional activity
Nakamura, Hiroyuki,Yasui, Yuka,Ban, Hyun Seung
, p. 189 - 194 (2013/11/19)
ortho-Carborane and adamantane containing benzoxazoles were synthesized by intramolecular dehydration of the corresponding phenoxyacetanilides. Among the compounds synthesized, ortho-carborane containing benzoxazole 2b which has a carboxylic group on the benzoxazole ring, exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity with the IC50 value of 14.4 μM toward HeLa cell-based reporter gene assay.
3,3′-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding
Weiser, Patrick T.,Williams, Anna B.,Hanson, Robert N.,Chang, Ching-Yi,McDonnell, Donald P.
, p. 6587 - 6590,4 (2012/12/12)
A series of bipolar biphenyl compounds was synthesized as proteomimetic analogs of the LXXLL penta-peptide motif responsible for the binding of coactivator proteins to the nuclear hormone receptor coactivator binding domain. These compounds were subjected
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
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.
Synthesis and properties of a novel type of acyclic nucleoside phosphonates: 2-(purin-9-yl)ethoxyphenylphosphonic acids
Hockova, Dana,Dracinsky, Martin,Holy, Antonin
scheme or table, p. 2885 - 2892 (2010/08/05)
A series of novel acyclic nucleoside phosphonates with a built-in arylphosphonate moiety has been prepared by a microwave-assisted cross-coupling reaction as the key step. Their cytostatic and antiviral activities were tested. The pKa values of the target ortho-, meta- and para-substituted arylphosphonates were determined by 31P NMR titration studies.
Sensitized emission of luminescent lanthanide complexes based on a phosphane oxide derivative
Ha-Thi, Minn-Huong,Delaire, Jacques Alexis,Michelet, Veronique,Leray, Isabelle
body text, p. 3264 - 3269 (2010/08/13)
The photophysical properties of a complex based on diphenylphosphanoethane (DPPE) fluorescent ligands linked to a europium ion have been investigated by different spectroscopic methods. Upon complexation with europium, the interaction of the phosphane oxi
Synthesis of biphenyl proteomimetics as estrogen receptor-a coactivator binding inhibitors
Williams, Anna B.,Weiser, Patrick T.,Hanson, Robert N.,Guenther, Julian R.,Katzenellenbogen, John A.
supporting information; experimental part, p. 5370 - 5373 (2010/02/28)
"Chemical Equation Presented" A novel series of blphenyl proteomlmetic compounds were designed as estrogen receptor-α (ERα) coactivator binding Inhibitors. Synthesis was accomplished through a convergent approach, employing Suzuki coupling chemistry to li
MODULATORS OF NUCLEAR RECEPTOR CO-REGULATORY PROTEIN BINDING
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Page/Page column 65, (2009/10/22)
Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.
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.
