Afficher la couverture 'Potassium 6-Oxo-7,13,16,22-tetraazatetracyclo[12.6.2.18,12.017,21]tricosa-1(20),8(23),9,11,14,16,18,21-octaen-2-yne-15-carboxylate | Blouet, Camille' en grand format
/5

0 avis

Potassium 6-Oxo-7,13,16,22-tetraazatetracyclo[12.6.2.18,12.017,21]tricosa-1(20),8(23),9,11,14,16,18,21-octaen-2-yne-15-carboxylate

Archive ouverte

Blouet, Camille | Letast, Stéphanie | Robert, Thomas | Bach, Stéphane | Pinaud, Noël | Joubert, Nicolas | Viaud-Massuard, Marie-Claude | Guillon, Jean | Logé, Cédric | Denevault-Sabourin, Caroline

Edité par CCSD ; MDPI -

International audience. Potassium 6-oxo-7,13,16,22-tetraazatetracyclo[12.6.2.18,12.017,21]tricosa-1(20),8(23),9,11,14,16,18,21-octaen-2-yne-15-carboxylate was synthesized through a multi-step pathway, starting from commercially available 3-iodo-1,2-phenylenediamine. Structure characterization of this new substituted macrocyclic quinoxaline compound was achieved using 1H NMR, 13C NMR, and HRMS spectral analysis. This new macrocyclic derivative demonstrated submicromolar potency on both Pim-1 and Pim-2 isoforms, with an interesting selectivity profile against a selected panel of human kinases.

Suggestions

Du même auteur

New Quinoxaline Derivatives as Dual Pim-1/2 Kinase Inhibitors: Design, Synthesis and Biological Evaluation

Archive ouverte | Oyallon, Bruno | CCSD

International audience. Proviral integration site for Moloney murine leukemia virus (Pim)-1/2 kinase overexpression has been identified in a variety of hematologic (e.g., multiple myeloma or acute myeloid leukemia (...

Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors

Archive ouverte | Oyallon, Bruno | CCSD

International audience. We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human proviral integration site for Moloney murine leukemia virus-1 (HsPim-1) kinase. Seventeen analogue...

Dual intra- and extracellular release of monomethyl auristatin E from a neutrophil elastase-sensitive antibody-drug conjugate

Archive ouverte | Mohamed Amar, Imene Ait | CCSD

International audience. Antibody-drug conjugates (ADCs) are targeted therapies, mainly used in oncology, consisting in a three-component molecular architecture combining a highly potent drug conjugated via a linker ...

Chargement des enrichissements...