Efficient synthesis of novel disubstituted pyrido[3,4-b]pyrazines for the design of protein kinase inhibitors

Autor: Pascal Marchand, Matthias Gerlach, Irene Seipelt, Michael Teifel, Maud Antoine, Eckhard Günther, Tilmann Schuster, Babette Aicher

Publikováno v: MedChemComm. 7:224-229

A novel family of disubstituted pyrido[3,4-b]pyrazine-based compounds was discovered as valuable series for the design of promising protein kinase inhibitors. SAR study allowed the identification of 4-(piperidin-1-yl)aniline moiety as pharmacophoric

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1ad15c5439e61e64968bf7d8a9749710
https://doi.org/10.1039/c5md00424a

Discovery of 7-Aryl-Substituted (1,5-Naphthyridin-4-yl)ureas as Aurora Kinase Inhibitors

Autor: Tilmann Schuster, Maud Antoine, Irene Seipelt, Marc Le Borgne, Babette Aicher, Michael Teifel, Eckhard Günther, Pascal Marchand, Julien Defaux, Matthias Gerlach

Publikováno v: ChemMedChem. 9:217-232

As part of our research projects to identify new chemical entities of biological interest, we developed a synthetic approach and the biological evaluation of (7-aryl-1,5-naphthyridin-4-yl)ureas as a novel class of Aurora kinase inhibitors for the tre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3354459e0908068066522bbf86a3a95
https://doi.org/10.1002/cmdc.201300384

New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center

Autor: Jean Martinez, Babette Aicher, Peter Schmidt, Jacky Marie, Jean-Louis Banères, Gilbert Müller, Sophie Mary, Anne-Laure Blayo, Didier Gagne, Séverine Denoyelle, Eckhard Günther, Mathieu Maingot, Michael Teifel, Céline M'Kadmi, Jean-Alain Fehrentz, Marjorie Damian, Pierre Sanchez

Publikováno v: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2016, 26 (10), pp.2408-2412. ⟨10.1016/j.bmcl.2016.04.003⟩

Introducing a second chiral center on our previously described 1,2,4-triazole, allowed us to increase diversity and elongate the 'C-terminal part' of the molecule. Therefore, we were able to explore mimics of the substance P analogs described as inve

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2453d99aed9b729a5b8511691d7dca67
https://hal.archives-ouvertes.fr/hal-02871896

Preparation of Novel 2,3,8-Trisubstituted Pyrido[3,4-b]pyrazines and Pyrido[2,3-b]pyrazines

Autor: Maud Antoine, Michael P. Czech, Matthias Gerlach, Pascal Marchand, Tilmann Schuster, Eckhard Günther

Publikováno v: Synthesis. 2011:794-806

A four-step synthesis of 8-bromo-2,3-disubstituted pyrido[3,4-b]pyrazines and a six-step synthesis of 8-amino-2,3-disub-stituted pyrido[3,4-b]pyrazines have been developed. A particularly valuable feature of this synthetic route is the possibility to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d0ce0a47eef97fd15560f6f5f8e6bc37
https://doi.org/10.1055/s-0030-1259429

Synthesis and structure–activity relationships of N-aryl(indol-3-yl)glyoxamides as antitumor agents

Autor: Guillaume Le Baut, Maud Antoine, Eckhard Günther, Michael P. Czech, Silke Baasner, Pascal Marchand

Publikováno v: Bioorganic & Medicinal Chemistry. 17:6715-6727

The synthesis and study of the structure-activity relationships of cytotoxic compounds based on N-pyridinyl or N-aryl-2-(1-benzylindol-3-yl)glyoxamide skeleton, represented by the lead structures D-24241 and D-24851, are described. The presence of N-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d886b5148e0556f928bf0aac069509f
https://doi.org/10.1016/j.bmc.2009.07.048