- Vinylboronic Acids as Efficient Bioorthogonal Reactants for Tetrazine Labeling in Living Cells
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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
- Eising, Selma,Van Der Linden, Nicole G. A.,Kleinpenning, Fleur,Bonger, Kimberly M.
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p. 982 - 986
(2018/04/23)
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- Synthesis and biological evaluation of ortho-carborane containing benzoxazole as an inhibitor of hypoxia inducible factor (HIF)-1 transcriptional activity
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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.
- Nakamura, Hiroyuki,Yasui, Yuka,Ban, Hyun Seung
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p. 189 - 194
(2013/11/19)
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- 3,3′-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding
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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
- Weiser, Patrick T.,Williams, Anna B.,Hanson, Robert N.,Chang, Ching-Yi,McDonnell, Donald P.
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p. 6587 - 6590,4
(2012/12/12)
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- Discovery of carboranes as inducers of 20S proteasome activity
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(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
- Ban, Hyun Seung,Minegishi, Hidemitsu,Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Nakamura, Hiroyuki
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experimental part
p. 1236 - 1241
(2011/02/21)
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- Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors
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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.
- Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Minegishi, Hidemitsu,Ban, Hyun Seung,Nakamura, Hiroyuki
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scheme or table
p. 1453 - 1456
(2010/07/06)
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- Synthesis and properties of a novel type of acyclic nucleoside phosphonates: 2-(purin-9-yl)ethoxyphenylphosphonic acids
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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.
- Hockova, Dana,Dracinsky, Martin,Holy, Antonin
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scheme or table
p. 2885 - 2892
(2010/08/05)
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- Sensitized emission of luminescent lanthanide complexes based on a phosphane oxide derivative
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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
- Ha-Thi, Minn-Huong,Delaire, Jacques Alexis,Michelet, Veronique,Leray, Isabelle
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body text
p. 3264 - 3269
(2010/08/13)
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- Synthesis of biphenyl proteomimetics as estrogen receptor-a coactivator binding inhibitors
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"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
- Williams, Anna B.,Weiser, Patrick T.,Hanson, Robert N.,Guenther, Julian R.,Katzenellenbogen, John A.
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supporting information; experimental part
p. 5370 - 5373
(2010/02/28)
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- MODULATORS OF NUCLEAR RECEPTOR CO-REGULATORY PROTEIN BINDING
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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.
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Page/Page column 65
(2009/10/22)
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- 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
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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.
- 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
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scheme or table
p. 7061 - 7064
(2009/11/30)
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- (Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors
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Structural modification of a compound discovered during screening using an HRE-dependent reporter assay has revealed a novel class of HIF-1 inhibitors, which potently inhibit the HIF-1α protein accumulation and its target gene expression under hypoxic conditions in human hepatocellular carcinoma Hep3B cells.
- Lee, Kyeong,Lee, Jeong Hyung,Boovanahalli, Shanthaveerappa K.,Jin, Yinglan,Lee, Mijeoung,Jin, Xuejun,Kim, Jin Hwan,Hong, Young-Soo,Lee, Jung Joon
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p. 1675 - 1684
(2008/02/01)
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- NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
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This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, inflammatory disease of the joints, neuropathies, HIV-related neuropathy, nerve injury, neurodegeneration, stroke, urinary bladder hypersensitivity including urinary incontinence, cystitis, stomach duodenal ulcer, irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD), fecal urgency, gastro-esophageal reflux disease (GERD), Crohn's disease, asthma, chronic obstructive pulmonary disease, cough, neurotic/allergic/inflammatory skin disease, psoriasis, pruritus, prurigo, irritation of skin, eye or mucous membrane, hyperacusis, tinnitus, vestibular hypersensitivity, episodic vertigo, cardiac diseases such as myocardial ischemia, hair growth-related disorders such as effluvium, alopecia, rhinitis, and pancreatitis.
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Page/Page column 78-79
(2010/11/28)
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- Synthesis and luminescence of novel EuIII complexing agents and labels with 4-(phenylethynyl)pyridine subunits
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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.
- Takalo, Harri,Hemmilae, Ilkka,Sutela, Timo,Latva, Martti
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p. 789 - 802
(2007/10/03)
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