- A Chan-Evans-Lam approach to trisubstituted vinyl ethers
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Trisubstituted vinyl ethers were accessedviaChan-Evans-Lam coupling of vinyl trifluoroborates and primary aliphatic alcohols. This approach complements prior methods that required the use of neat liquid alcohol coupling partners. A palladium-catalyzed redox-relay Heck reaction was used to convert several vinyl ethers into aldehyde-functionalized 1,3-dihydroisobenzofurans.
- Molder, Bryce A.,Sader, Jonathan K.,Wulff, Jeremy E.
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supporting information
p. 9649 - 9653
(2021/12/01)
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- Synthesis of a triethylene glycol-capped benzo[1,2-c:4,5-c']bis[2]benzopyran-5,12-dione: A highly soluble dilactone-bridged p-terphenyl with a crankshaft architecture
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3,10-Bis(triethylene glycol)benzo[1,2-c:4,5-c']bis[2]benzopyran-5,12-dione has been synthesized as an example of a dilactone-bridged p-terphenyl with a C2h crankshaft architecture that exhibits significant fluorescence. Lactone-bridged rotation
- Dressler, Justin J.,Charlesworth-Seiler, Eva M.,Dahl, Bart J.
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supporting information
(2020/10/02)
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- Near infrared fluorescent probe capable of being used for responding to pH change in living cells in chronic wound development process and preparation method of probe
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The invention discloses a near infrared fluorescent probe capable of being used for responding to the pH change in living cells in the chronic wound development process and a preparation method of theprobe, and belongs to the technical field of biological
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Paragraph 0039; 0041; 0043-0045
(2019/06/07)
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- A pH-sensitive near-infrared fluorescent probe with alkaline p: K a for chronic wound monitoring in diabetic mice
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A pH-sensitive near-infrared fluorescent probe with alkaline pKa, AlkaP-1, was developed by incorporating a benzoyl hydrazine group into a cyanine dye. The significant fluorescence changes in the alkaline regions enable the probe to monitor the alkalization process from acute wounds to chronic wounds in diabetic mice.
- Mai, Hengtang,Wang, Yu,Li, Shuang,Jia, Ruizhen,Li, Sixian,Peng, Qian,Xie, Yan,Hu, Xiang,Wu, Song
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supporting information
p. 7374 - 7377
(2019/06/27)
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- Concise Synthesis of a Potential 5-Lipoxygenase Activating Protein (FLAP) Inhibitor and Its Analogs through Late-Stage Alkene Dicarbofunctionalization
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We report a five-step synthesis of the biologically important 1,1-diarylalkane 1, a potential 5-lipoxygenase activating protein (FLAP) inhibitor that was synthesized previously in 12 steps. In this synthesis, we apply a three-component alkene dicarbofunct
- Kc, Shekhar,Dhungana, Roshan K.,Aryal, Vivek,Giri, Ramesh
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p. 1686 - 1694
(2019/07/04)
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- Structure-Based Approach to Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators
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In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound 7, a potent AR (ARE EC50 = 0.34 nM) and selective (N/C interaction EC50 = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of 7, and further insights from modeling studies of ligand receptor interactions are also presented.
- Unwalla, Ray,Mousseau, James J.,Fadeyi, Olugbeminiyi O.,Choi, Chulho,Parris, Kevin,Hu, Baihua,Kenney, Thomas,Chippari, Susan,McNally, Christopher,Vishwanathan, Karthick,Kilbourne, Edward,Thompson, Catherine,Nagpal, Sunil,Wrobel, Jay,Yudt, Matthew,Morris, Carl A.,Powell, Dennis,Gilbert, Adam M.,Chekler, Eugene L. Piatnitski
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supporting information
p. 6451 - 6457
(2017/08/02)
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- Ruthenium-Catalyzed Hydroarylation and One-Pot Twofold Unsymmetrical C?H Functionalization of Arenes
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A methyl phenyl sulfoximine (MPS) is used as a directing group in the ruthenium-catalyzed intramolecular hydroarylation of alkene-tethered benzoic acid derivatives to afford dihydrobenzofurans and indolines in good to excellent yields. A one-pot, unsymmetrical, twofold C?H functionalization involving intramolecular C?C and intermolecular C?C/C?N bond formations is successfully demonstrated by using a single set of catalytic reaction conditions, which is unprecedented thus far. A novel isoquinolone-bearing dihydrobenzofuran is constructed through an unsymmetrical twofold C?H functionalization.
- Ghosh, Koushik,Ramesh, E.,Rit, Raja K.,Sahoo, Akhila K.
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supporting information
p. 7821 - 7825
(2016/07/07)
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- NOVEL CHARTREUSIN ANALOGUES
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The present invention relates to novel Chartreusin analogues of formula (I), pharmaceutical compositions comprising the same and to their use for the treatment of cancer and other diseases.
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Page/Page column 15; 16; 36
(2014/02/16)
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- Synthetic remodeling of the chartreusin pathway to tune antiproliferative and antibacterial activities
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Natural products of the benzonaphthopyranone class, such as chartreusin, elsamicin A, gilvocarcin, and polycarcin, represent potent leads for urgently needed anticancer therapeutics and antibiotics. Since synthetic protocols for altering their architectur
- Ueberschaar, Nico,Xu, Zhongli,Scherlach, Kirstin,Metsae-Ketelae, Mikko,Bretschneider, Tom,Dahse, Hans-Martin,Goerls, Helmar,Hertweck, Christian
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supporting information
p. 17408 - 17416
(2014/01/06)
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- ISOQUINOLINE COMPOUNDS AND METHODS FOR TREATING HIV
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Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
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- SUBSTITUTED 5-AMINOPYRAZOLES AND USE THEREOF
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The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases.
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Page/Page column 94-95
(2010/04/03)
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- NOVEL COMPOSITIONS AND METHODS OF USE
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Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.
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Page/Page column 165
(2009/09/04)
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- CARBAMOYL-SUBSTITUTED SPIRO DERIVATIVE
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A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent -C(O)-, etc.; Q represents a methine or a nitrogen; and R represents the formula
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Page/Page column 90
(2008/06/13)
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- NOVEL COMPOUNDS
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The present invention relates to novel phenylalanine compounds, processes for their preparation, compositions comprising them and their use in the treatment or prevention of diseases capable of being modulated by the inhibition of cell adhesion.
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Page/Page column 21; 26-27
(2010/02/12)
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- ANILINOPYRAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DIABETES
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The present invention relates to anilinopyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
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- ACID AND ESTER COMPOUNDS AND METHODS OF USING THE SAME
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Disclosed is a compound of having the formula (II-A), pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.
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Page/Page column 70
(2008/06/13)
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