AI Article Synopsis
- A high throughput screening of corporate compounds uncovered a new series of selective progesterone receptor (PR) agonists.
- Initial structure-activity relationship (SAR) studies focused on identifying potent compounds led to the promising discoveries of agonists 9 and 11.
- The study includes the X-ray crystal structure of compound 9 bound to the PR-ligand binding domain along with some early development data.
Article Abstract
High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective PR agonists. Initial SAR exploration leading to potent and selective agonists 9 and 11, X-ray crystal structure of 9 bound to PR-LBD and preliminary developability data are described.
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| http://dx.doi.org/10.1016/j.bmcl.2009.07.100 | DOI Listing |
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