- A diphenylphosphinoethane-functionalized polystyrene resin-supported Pd(0) complex as an effective catalyst for copper-free Sonogashira coupling reactions under aerobic conditions
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A polymer-supported palladium(0) diphenylphosphinoethane complex was found to be a highly active catalyst for the copper-free Sonogashira coupling reaction of aryl iodides with terminal alkynes, giving excellent yields of products (85-98%) under aerobic c
- Bakherad, Mohammad,Keivanloo, Ali,Bahramian, Bahram,Mihanparast, Samira
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Read Online
- Optical Control of Mitosis with a Photoswitchable Eg5 Inhibitor
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Eg5 is a kinesin motor protein that is responsible for bipolar spindle formation and plays a crucial role during mitosis. Loss of Eg5 function leads to the formation of monopolar spindles, followed by mitotic arrest, and subsequent cell death. Several cell-permeable small molecules have been reported to inhibit Eg5 and some have been evaluated as anticancer agents. We now describe the design, synthesis, and biological evaluation of photoswitchable variants with five different pharmacophores. Our lead compound Azo-EMD is a cell permeable azobenzene that inhibits Eg5 more potently in its light-induced cis form. This activity decreased the velocity of Eg5 in single-molecule assays, promoted formation of monopolar spindles, and led to mitotic arrest in a light dependent way.
- Impastato, Anna C.,Shemet, Andrej,Vep?ek, Nynke A.,Saper, Gadiel,Hess, Henry,Rao, Lu,Gennerich, Arne,Trauner, Dirk
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supporting information
(2022/01/20)
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- Applications of Thermal Activation, Ball-milling and Aqueous Medium in Stereoselective Michael Addition of Nitromethane to Enynones Catalyzed by Chiral Squaramides
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Stereoselective addition of nitromethane to conjugated en-ynones was performed through the application of chiral squaramides. Three non-classical approaches to promote the addition reaction were tested, including activation of the nucleophile by inorganic base in a biphasic aqueous system, thermal activation, and ball-milling. Hydrogen-bonding catalysis was effective in all these methods, providing 1,4-addition products in high yields and stereoselectivities of up to 98% requiring 1–5 mol% of Cinchona alkaloid squaramide. (Figure presented.).
- Ignatiuk, ?aneta A.,Janicki, Miko?aj J.,Góra, Robert W.,Konieczny, Krzysztof,Kowalczyk, Rafa?
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supporting information
p. 1108 - 1116
(2019/01/30)
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- Neighboring Carbonyl Group Assisted Hydration of Unsymmetrical Aryl Alkynes Overriding Regular Selectivity
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A mild and highly regioselective gold-catalyzed hydration of γ-acetoxy aryl alkynes leading to anti-Markovnikov products by the assistance of a neighboring carbonyl group is presented. The reaction procedure operates under room temperature conditions with
- Mendhekar, Kishor L.,Pradhan, Tapas R.,Mallampudi, N. Arjunreddy,Mohapatra, Debendra K.
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p. 5787 - 5797
(2019/08/21)
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- Ligand-Controlled Regioselective Copper-Catalyzed Trifluoromethylation To Generate (Trifluoromethyl)allenes
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(Chemical Equation Presented) "Cu-CF3" species have been used historically for a broad spectrum of nucleophilic trifluoromethylation reactions. Although recent advancements have employed ligands to stabilize and harness the reactivity of this key organometallic intermediate, the ability of a ligand to differentiate a regiochemical outcome of a Cu-CF3-mediated or -catalyzed reaction has not been previously reported. Herein, we report the first example of a Cu-catalyzed trifluoromethylation reaction in which a ligand controls the regiochemical outcome. More specifically, we demonstrate the ability of bipyridyl-derived ligands to control the regioselectivity of the Cu-catalyzed nucleophilic trifluoromethylation reactions of propargyl electrophiles to generate (trifluoromethyl)allenes. This method provides a variety of di-, tri-, and tetrasubstituted (trifluoromethyl)allenes, which can be further modified to generate complex fluorinated substructures.
- Ambler, Brett R.,Peddi, Santosh,Altman, Ryan A.
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supporting information
p. 2506 - 2509
(2015/05/27)
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- Copper-free Sonogashira coupling reactions catalyzed by a water-soluble Pd-salen complex under aerobic conditions
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The water-soluble Pd-salen complex, palladium(II) N,N′-bis{[5-(triphenylphosphonium)methyl]salicylidene}-1,2-ethanediamine chloride, is a highly active catalyst for the copper-free Sonogashira coupling of aryl iodides with terminal alkynes in water under
- Bakherad, Mohammad,Keivanloo, Ali,Bahramian, Bahram,Hashemi, Mahdieh
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experimental part
p. 1557 - 1559
(2009/06/21)
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- Optimized N-phenyl-N′-(2-chloroethyl)ureas as potential antineoplastic agents: Synthesis and growth inhibition activity
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In our ongoing research program aimed at the optimization of microtubule-self-assembly disrupting agents, we have prepared three series of phenylurea analogues (CEU), derived from N-(3-ω-hydroxyalkyl or 4-ω-hydroxyalkyl or 3-ω-hydroxyalkynyl)-phenyl-N′-(2
- Moreau, Emmanuel,Fortin, Sebastien,Desjardins, Michel,Rousseau, Jean L.C.,Petitclerc, Eric,C.-Gaudreault, Rene
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p. 6703 - 6712
(2007/10/03)
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- HALOETHYL UREA COMPOUNDS AND THEIR USE TO ATTENUATE, INHIBIT OR PREVENT NON-CANCEROUS PATHOGENIC CELLULAR PROLIFERATION AND DISEASES ASSOCIATED THEREWITH
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The present invention provides haloethyl urea compounds as described in Formula (I) and their use as anti-proliferative agent in the attenuation, inhibition, or prevention of non-cancerous cellular proliferation. These compounds are also provided for use as a therapeutic agent in the treatment of a disease or disorder, wherein pathogenesis of said disease or disorder is associated with non-cancerous pathogenic cellular proliferation.
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Page 78-79; 85-86
(2010/02/09)
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- HALOETHYL UREA COMPOUNDS AND THE USE THEREOF TO ATTENUATE, INHIBIT OR PREVENT CANCER CELL MIGRATION
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The present invention provides haloethyl urea compounds as described in Formula (I) and their use as therapeutic agent in the attenuation, inhibition, or prevention of cancer cell migration and cancer cell proliferation.
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Page 75; 76; 82
(2010/02/09)
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- Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)- 1-azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)-oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist
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The synthesis and SAR of a series of (Z)-(±)-1- azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl)oximes are described. The biochemistry and pharmacology of 24Z (PD 142505) and its enantiomers are highlighted. 24Z is functionally an m1-selective muscari
- Tecle, Halle,Barrett, Stephen D.,Lauffer, David J.,Augelli-Szafran, Corinne,Brann, Mark R.,Callahan, Michael J.,Caprathe, Bradley W.,Davis, Robert E.,Doyle, Patricia D.,Eubanks, David,Lipiniski, William,Mirzadegan, Tara,Moos, Walter H.,Moreland,Nelson, Carrie B.,Pavia, Michael R.,Raby, Charlotte,Schwarz, Roy D.,Spencer, Carolyn J.,Thomas, Anthony J.,Jaen, Juan C.
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p. 2524 - 2536
(2007/10/03)
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