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Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: A template-based approach |
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| Authors: | Michael P. Dwyer Kartik Keertikar Kamil Paruch Carmen Alvarez Marc Labroli Cory Poker Thierry O. Fischmann Rosemary Mayer-Ezell Richard Bond Yan Wang Rita Azevedo Timothy J. Guzi |
| Affiliation: | 1. Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States;2. Department of Tumor Biology, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States;3. Molecular Design and Informatics, Oss 5340 BH, The Netherlands |
| Abstract: | The synthesis and hit-to-lead SAR development from a pyrazolo[1,5-a]pyrimidine-derived hit 5 to the identification of a series of potent, pan–Pim inhibitors such as 11j are described. |
| Keywords: | Pan–Pim kinase |
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