Structure-based optimization of aminothiadiazole inhibitors of AKT
Author:
Publisher
Springer Science and Business Media LLC
Subject
Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics
Link
https://link.springer.com/content/pdf/10.1007/s00044-023-03072-4.pdf
Reference14 articles.
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2. Dumble M, Crouthamel M-C, Zhang S-Y, Schaber M, Levy D, Robell K, et al. Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor. PLoS ONE. 2014;9:e100880 https://doi.org/10.1371/journal.pone.0100880.
3. Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013;19:1760–72. https://doi.org/10.1158/1078-0432.CCR-12-3072.
4. Davies BR, Greenwood H, Dudley P, Crafter C, Yu DH, Zhang J, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012;11:873–87. https://doi.org/10.1158/1535-7163.MCT-11-0824-T.
5. Politz O, Siegel F, Bärfacker L, Bömer U, Hägebarth A, Scott WJ, et al. BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. Int J Cancer. 2017;140:449–59. https://doi.org/10.1002/ijc.30457.
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