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Structure-based optimization of potent PDK1 inhibitors |
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| Authors: | Mauro Angiolini Patrizia Banfi Elena Casale Francesco Casuscelli Claudio Fiorelli Maria B. Saccardo Marco Silvagni Fabio Zuccotto |
| Affiliation: | Nerviano Medical Sciences Srl, Viale Pasteur 10, 20014 Nerviano, Milano, Italy |
| Abstract: | In this Letter is described the structure-based design of potent dihydro-pyrazoloquinazolines as PDK1 inhibitors. Starting from low potency HTS hits with the aid of X-ray crystallography and modeling, a medicinal chemistry activity was carried out to improve potency versus PDK1 and selectivity versus CDK2 protein kinase. |
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