AI Article Synopsis
- The text discusses the development of selective dual mTORC1 and mTORC2 inhibitors, focusing on enhancing cellular potency while improving solubility and safety profiles.
- The initial results led to the identification of AZD8055 as a strong clinical candidate.
- Further refinement aimed at decreasing metabolism rates in human liver cells resulted in another promising candidate, AZD2014.
Article Abstract
The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency whilst maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC(50), led to the discovery of the clinical candidate AZD8055 (14). Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014 (21).
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| http://dx.doi.org/10.1016/j.bmcl.2013.01.019 | DOI Listing |
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