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. 2010 Mar 1;20(5):1652-6.
doi: 10.1016/j.bmcl.2010.01.046. Epub 2010 Jan 20.

2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics

Qingping Zeng  1 , Matthew P Bourbeau, G Erich Wohlhieter, Guomin Yao, Holger Monenschein, James T Rider, Matthew R Lee, Shiwen Zhang, Julie Lofgren, Daniel Freeman, Chun Li, Elizabeth Tominey, Xin Huang, Douglas Hoffman, Harvey Yamane, Andrew S Tasker, Celia Dominguez, Vellarkad N Viswanadhan, Randall Hungate, Xiaoling Zhang
Affiliations

2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics

Qingping Zeng et al. Bioorg Med Chem Lett. .

Abstract

A series of 2-aminothiadiazole of inhibitors of AKT1 is described. SAR relationships are discussed, along with selectivity for protein kinase A (PKA) and cyclin-dependent kinase 2 (CDK2). Moderate selectivity observed in several compounds for AKT1 versus PKA is rationalized by X-ray crystallographic analysis. Key compounds showed activity in cellular assays measuring phosphorylation of two AKT substrates, PRAS40 and FKHRL1. Compound 30 was advanced to a mouse liver PD assay, where it showed dose-dependent inhibition of AKT activity, as measured by the inhibition of phospho-PRAS40.

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