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Dr. Christopher R. M. Asquith Dr. Tuomo Laitinen James M. Bennett Carrow I. Wells Dr. Jonathan M. Elkins Dr. William J. Zuercher Dr. Graham J. Tizzard Prof. Antti Poso 《ChemMedChem》2020,15(1):26-49
The 4-anilinoquinoline and 4-anilinoquinazoline ring systems have been the focus of significant efforts in prior kinase drug discovery programs, which have led to approved medicines. Broad kinome profiles of these compounds have now been assessed with the advent of advanced screening technologies. These ring systems, while originally designed for specific targets including epidermal growth factor receptor (EGFR), but actually display a number of potent collateral kinase targets, some of which have been associated with negative clinical outcomes. We have designed and synthesized a series of 4-anilinoquin(az)olines in order to better understand the structure-activity relationships of three main collateral kinase targets of quin(az)oline-based kinase inhibitors: cyclin G associated kinase (GAK), STE20-like serine/threonine-protein kinase (SLK) and serine/threonine-protein kinase 10 (STK10). This was achieved through a series of quantitative structure-activity relationship (QSAR) analysis, water mapping of the kinase ATP binding sites and extensive small-molecule X-ray structural analysis. 相似文献
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Front Cover: Alanine and Lysine Scans of the LL‐37‐Derived Peptide Fragment KR‐12 Reveal Key Residues for Antimicrobial Activity (ChemBioChem 9/2018) 下载免费PDF全文
Dr. Sunithi Gunasekera Taj Muhammad Dr. Adam A. Strömstedt Dr. K. Johan Rosengren Prof. Dr. Ulf Göransson 《Chembiochem : a European journal of chemical biology》2018,19(9):891-891