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17 results on '"Suppo, Jean-Simon"'

2. Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition

Author

Universitat Rovira i Virgili, Wu, Zhenhua; Suppo, Jean-Simon; Tumova, Sarka; Strope, Jonathan; Bravo, Fernando; Moy, Melody; Weinstein, Ethan S.; Peer, Cody J.; Figg, William D.; Chain, William J.; Echavarren, Antonio M.; Beech, David J.; Beutler, John A., Universitat Rovira i Virgili, and Wu, Zhenhua; Suppo, Jean-Simon; Tumova, Sarka; Strope, Jonathan; Bravo, Fernando; Moy, Melody; Weinstein, Ethan S.; Peer, Cody J.; Figg, William D.; Chain, William J.; Echavarren, Antonio M.; Beech, David J.; Beutler, John A.

Abstract

Modifications at the bridgehead position of englerin A were made to explore the effects of variation at this site on the molecule for biological activity, as judged by the NCI 60 screen, in which englerin A is highly potent and selective for renal cancer cells. Replacement of the isopropyl group by other, larger substituents yielded compounds which displayed excellent selectivity and potency comparable to the natural product. Selected compounds were also evaluated for their effect on the ion channel TRPC4 as well as for intravenous toxicity in mice, and these had lower potency in both assays compared to englerin A.

Published
2020

3. Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition

Author

Wu, Zhenhua, primary, Suppo, Jean-Simon, additional, Tumova, Sarka, additional, Strope, Jonathan, additional, Bravo, Fernando, additional, Moy, Melody, additional, Weinstein, Ethan S., additional, Peer, Cody J., additional, Figg, William D., additional, Chain, William J., additional, Echavarren, Antonio M., additional, Beech, David J., additional, and Beutler, John A., additional

Published
2020
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5. Dipeptide Syntheses via Activated α-Aminoesters

Author

Suppo, Jean-Simon, Marcia De Figueiredo, Renata, Campagne, Jean-Marc, Institut Charles Gerhardt Montpellier - Institut de Chimie Moléculaire et des Matériaux de Montpellier (ICGM ICMMM), Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Institut de Chimie du CNRS (INC), and ANR-12-JS07-0008,NIPS,Développement d'une nouvelle stratégie pour la synthèse peptidique inversée(2012)

Subjects
[CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Organic Chemistry, Physical and Theoretical Chemistry, 010402 general chemistry, 01 natural sciences, ComputingMilieux_MISCELLANEOUS, 0104 chemical sciences
Abstract

International audience

Published
2015

6. Sequential One-Pot Synthesis of Dipeptides through the Transient Formation of CDI-N--Protected alpha--Aminoesters

Author

Marcia De Figueiredo, Renata, Suppo, Jean-Simon, Midrier, Camille, Campagne, Jean-Marc, Institut Charles Gerhardt Montpellier - Institut de Chimie Moléculaire et des Matériaux de Montpellier (ICGM ICMMM), and Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Institut de Chimie du CNRS (INC)

Subjects
atom economy, amide bond formation, [CHIM.ORGA]Chemical Sciences/Organic chemistry, dipeptides, base-free procedure, non-activated carboxylic acids, ComputingMilieux_MISCELLANEOUS
Abstract

International audience

Published
2017

17. Efficient and Practical Procedure for the Esterification of the Free α-Carboxylic Acid of Amino Acid Residues with β-(Trimethylsilyl)ethoxymethyl Chloride and Triisopropylsilyl Chloride.

Author

Suppo, Jean-Simon, de Sant'Ana, Danilo Pereira, Dias, Luiz Carlos, de Figueiredo, Renata Marcia, and Campagne, Jean-Marc

Subjects
*ESTERIFICATION, *CARBOXYLIC acids, *AMINO acids, *CHLORIDES, *PEPTIDE synthesis
Abstract

An efficient and practical procedure for the free α-carboxylic acid esterification of amino acid residues with β-(trimethylsilyl) ethoxymethyl chloride and triisopropylsilyl chloride is described. The reaction takes place under mild conditions and the expected protected amino acids are obtained in good to excellent yields. Our method provides a useful alternative for the C-terminal carboxylic acid protection of amino acids and peptides. Moreover, the removal of such protection was also achieved under mild conditions, without affecting either the other protecting groups at the aamino moiety and side chains or the optical integrity at the α-position of the amino acid residues. Examples of their use in peptide synthesis are also illustrated. [ABSTRACT FROM AUTHOR]

Published
2014
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