Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH)

Autor: Laurent Meijer, Marie Knockaert, Anja Becker, Yoan Ferandin, Lutz Preu, Conrad Kunick, Simone Kohfeld, Karen Wieking, Annette Lader, Tanja Pies

Publikováno v: European Journal of Medicinal Chemistry. 45:335-342

A collection of paullones was tested for inhibitory activity against mitochondrial malate dehydrogenase (mMDH) as a biological target for antiproliferative activity. Based on the results of this screening, 5-benzylpaullones and paullone-9-carboxylic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a921d272b3946e5031b3e38dd7b4a9fe
https://doi.org/10.1016/j.ejmech.2009.10.018

Evaluation and Comparison of 3D-QSAR CoMSIA Models for CDK1, CDK5, and GSK-3 Inhibition by Paullones

Autor: Daniel W. Zaharevitz, Alexander Weber, C. Schultz, Rick Gussio, Flemming Jørgensen, Maryse Leost, Xu Xie, Conrad Kunick, Kathrin Lauenroth, Laurent Meijer, Thomas Lemcke, Karen Wieking

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2004, 47, pp.22-36
Journal of Medicinal Chemistry, 2004, 47, pp.22-36

With a view to the rational design of selective GSK-3beta inhibitors, 3D-QSAR CoMSIA models were developed for the inhibition of the three serine/threonine kinases CDK1/cyclin B, CDK5/p25, and GSK-3beta by compounds from the paullone inhibitor family

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c4c080411d0a6bc7e95d137925d6bf5
https://doi.org/10.1021/jm0308904

Biotin labelling of amines by polymer-assisted solution-phase synthesis

Autor: Andreas Link, Karen Wieking, Abolfasl Golisade, Conrad Kunick, Claudia Herforth

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:1783-1786

An efficient and simple polymer-assisted approach has been developed to biotinylate multifunctional compounds bearing an amino functionality. Biotin was immobilized on aminomethylated polystyrene via the Kenner safety catch linker, activated and subs

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0c2688c15a0184cf54f5f2542694160
https://doi.org/10.1016/s0960-894x(01)00296-7

ChemInform Abstract: Synthesis of 11H-Indolo[3,2-c]quinoline-6-carboxylic Acids by Cascade Autoxidation-Ring Contractions

Autor: Lutz Preu, Anja Becker, Tanja Pies, Karen Wieking, Simone Kohfeld, Conrad Kunick

Publikováno v: ChemInform. 40

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4f0dc02e402c90266f903fa5e3aa8a20
https://doi.org/10.1002/chin.200934150

Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor

Autor: Marie, Knockaert, Karen, Wieking, Sophie, Schmitt, Maryse, Leost, Karen M, Grant, Jeremy C, Mottram, Conrad, Kunick, Laurent, Meijer

Publikováno v: The Journal of biological chemistry. 277(28)

Numerous inhibitors of cyclin-dependent kinases and glycogen synthase kinase-3 (GSK-3) are being developed in view of their potential applications against cancers and neurodegenerative disorders. Among these, paullones constitute a family of potent a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::d787dd6d38ac1287552490b8557642d2
https://pubmed.ncbi.nlm.nih.gov/11964410