443770-52-3Relevant academic research and scientific papers
Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors
Robke, Lucas,Rodrigues, Tiago,Schr?der, Peter,Foley, Daniel J.,Bernardes, Gon?alo J.L.,Laraia, Luca,Waldmann, Herbert
supporting information, p. 4531 - 4537 (2018/07/30)
Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small molecule modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biological validation experiments indicated that the mode of action was upstream or independent of mTOR.
