Synthesis of enantiopure α-Tfm-proline and α-Tfm-pipecolic acid from oxazolo-pyrrolidines and -piperidines

Autor: Charlène Gadais, Evelyne Chelain, Nathalie Lensen, Thierry Brigaud, Sitan Diarra, Clément Sanchez, Andrea Bordessa

Publikováno v: Organic & Biomolecular Chemistry. 19:6771-6775

Enantiopure α-Tfm-proline and α-Tfm-pipecolic acid were synthesized starting from commercially available diesters and ethyl trifluoroacetate. A Strecker type reaction on intermediate chiral Tfm-oxazolo-pyrrolidine and -piperidine provided the corre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eb7f7454019c1346f66c7c839445ef8
https://doi.org/10.1039/d1ob01173a

Corrigendum to 'New desulfured troglitazone derivatives: Improved synthesis and biological evaluation' [Eur. J. Med. Chem. 187 (2020) 111939]

Autor: Elia de Fays, Hélène Martin, Michel Boisbrun, Stéphane Flament, Flavian Piquard, Eline Piquard, Claire Muller, Stéphanie Grandemange, Sabine Mazerbourg, Manon Pawlak, Andrea Bordessa, Dorian Dupommier, Corinne Comoy

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2020, 208, pp.112834. ⟨10.1016/j.ejmech.2020.112834⟩

International audience

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5bce2e178a8e4760c352980612d25359
https://hal.archives-ouvertes.fr/hal-03503731

Orthogonal 19 F-Labeling for Solid-State NMR Spectroscopy Reveals the Conformation and Orientation of Short Peptaibols in Membranes

Autor: Anne S. Ulrich, Stephan L. Grage, Grégory Chaume, Sergii Afonin, Andrea Bordessa, Fabio Rizzolo, Tomáš Kubař, Anna Maria Papini, Véronique Doan, Marina Putzu, Thierry Brigaud, Sezgin Kara

Publikováno v: Chemistry - A European Journal. 24:4328-4335

Peptaibols are promising drug candidates in view of their interference with cellular membranes. Knowledge of their lipid interactions and membrane-bound structure is needed to understand their activity and should be, in principle, accessible by solid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a458132d9e399dbec4608235ed0dbef6
https://doi.org/10.1002/chem.201704307

Reprofiling of Troglitazone Towards More Active and Less Toxic Derivatives: A New Hope for Cancer Treatment?

Autor: Marine Geoffroy, Andrea Bordessa, Michel Boisbrun, Sandra Kuntz, Stéphane Flament, Sabine Mazerbourg, Isabelle Grillier-Vuissoz, Audrey Berthe

Publikováno v: Current Topics in Medicinal Chemistry
Current Topics in Medicinal Chemistry, Bentham Science Publishers, 2016, 16 (19), pp.2115-2124. ⟨10.2174/1568026616666160216153036⟩

International audience; The existence of unresponsive tumors and the appearance of resistant tumors during the course of treatments both justify that we increase urgently the panel of pharmacological molecules able to fight cancer. An interesting str

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b54a8195cb9a4d1a7a969c39bf45948
https://doi.org/10.2174/1568026616666160216153036

Structural Behavior of the Peptaibol Harzianin HK VI in a DMPC Bilayer: Insights from MD Simulations

Autor: Stephan L. Grage, Andrea Bordessa, Grégory Chaume, Marina Putzu, Anne S. Ulrich, Sezgin Kara, Tomáš Kubař, Thierry Brigaud, Sergii Afonin

Microsecond molecular dynamics simulations of harzianin HK VI (HZ) interacting with a dimyristoylphosphatidylcholine bilayer were performed at the condition of low peptide-to-lipid ratio. Two orientations of HZ molecule in the bilayer were found and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::625785cdb7f901c8085b5904dd0ed5af
https://europepmc.org/articles/PMC5479149/