- Low dilution procedures in solid-phase organic synthesis: Diels-Alder and Heck reactions
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The use of extremely low solvent volumes (2 μL or less per mg resin) results in significant increases in yield for both the Diels-Alder and Heck reactions on solid-phase compared to standard high dilution techniques.
- Morphy, J.Richard,Rankovic, Zoran,York, Mark
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Read Online
- 5,6-dihydropyrrolo[2,1-a]isoquinolines as alternative of new drugs with cytotoxic activity
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In this study, the pyrrolo[2,1-a]isoquinolines 4a–n were synthesized in good yields in a three steps synthesis from the corresponding α,β-unsaturated esters starting materials. These compounds were tested on six human cancer cells lines to measure the cyt
- Chávez-Santos, Rosa María,Torres-Ochoa, Rubén Omar,Ramírez-Apan, María Teresa,Martínez, Roberto,Reyes-Gutiérrez, Paul Eduardo
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p. 973 - 981
(2018/11/02)
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- AROMATIC RING COMPOUND
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Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
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Paragraph 0320; 0321
(2015/01/18)
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- CLASS- AND ISOFORM-SPECIFIC HDAC INHIBITORS AND USES THEREOF
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HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and d
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Page/Page column 98
(2011/02/24)
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- HETEROCYCLIC COMPOUND
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The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
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Page/Page column 73-74
(2010/07/08)
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- Synthesis of 5,6-dihydropyrrolo[2,1-a]isoquinolines featuring an intramolecular radical-oxidative cyclization of polysubstituted pyrroles, and evaluation of their cytotoxic activity
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A three-step protocol for the synthesis of 1,2,3,8,9-pentasubstituted-5,6- dihydropyrrolo[2,1-a]isoquinolines is described, using van LeuseN′s polysubstituted pyrrole construction followed by intramolecular radical-oxidative cyclization of the isoquinoline system. The cytotoxic activities of the dihydropyrroloisoquinolines were tested on six tumor cell lines. Preliminary structure-activity studies revealed the importance of the identity of the aromatic substituent at the C-2 position, particularly a phenyl, m-(amino) phenyl or m-(cyclohexylmethylpiperazinamide) phenyl substituent, for cytotoxic activity.
- Reyes-Gutierrez, Paul E.,Camacho, Jose R.,Ramirez-Apan, Ma. Teresa,Osornio, Yazmin M.,Martinez, Roberto
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body text
p. 4374 - 4382
(2010/11/04)
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- Substituted benzamide inhibitors of rhinovirus 3C protease
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Nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease are described.
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Page column 12
(2010/01/31)
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- Substituted benzamide inhibitors of human rhinovirus 3C protease: Structure-based design, synthesis, and biological evaluation
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A series of nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease was identified using structure-based design. The design, synthesis, and biological evaluation of these inhibitors are reported. A Michael acceptor was combined with a benzamide core mimicking the P1 recognition element of the natural 3CP substrate, α,β-Unsaturated cinnamate esters irreversibly inhibited the 3CP and displayed antiviral activity (EC50 0.60/μM, HRV-16 infected H1-HeLa cells). On the basis of cocrystal structure information, a library of substituted benzamide derivatives was prepared using parallel synthesis on solid support. A 1.9 A? cocrystal structure of a benzamide inhibitor in complex with the 3CP revealed a binding mode similar to that initially modeled wherein covalent attachment of the nucleophilic cysteine residue is observed. Unsaturated ketones displayed potent reversible inhibition but were inactive in the cellular antiviral assay and were found to react with nucleophilic thiols such as DTT.
- Reich, Siegfried H.,Johnson, Theodore,Wallace, Michael B.,Kephart, Susan E.,Fuhrman, Shella A.,Worland, Stephen T.,Matthews, David A.,Hendrickson, Thomas F.,Chan, Fora,Meador III, James,Ferre, Rose Ann,Brown, Edward L.,DeLisle, Dorothy M.,Patick, Amy K.,Binford, Susan L.,Ford, Clifford E.
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p. 1670 - 1683
(2007/10/03)
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- SELECTIVE PREPARATION OF NON-SYMMETRICALLY SUBSTITUTED DIVINYLBENZENES BY PALLADIUM-CATALYSED ARYLATIONS OF ALKENES WITH BROMOBENZOIC ACID DERIVATIVES
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Palladium-catalysed arylation of alkenes with the three bromobenzoic acids or their acyl chlorides provides an efficient and selective method for the preparation of non-symmetrically substituted divinylbenzene derivatives.In the presence of palladium acet
- Spencer, Alwyn
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p. 323 - 332
(2007/10/02)
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