Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors |
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| Authors: | Zhaoyang Meng Jeffrey P. Ciavarri Andrew McRiner Yinyan Zhao Lianyun Zhao Panduranga Adulla Reddy Xingmin Zhang Thierry O. Fischmann Charles Whitehurst M. Arshad Siddiqui |
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| Affiliation: | 1. Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, USA;2. Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
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| Abstract: | Chemistry has been developed to access both imidazo[1,2-a]pyrazines and imidazo[1,2-c]pyrimidines. Small structural modifications in both series led to a switch of potency between two kinases involved in mediating cell cycle checkpoint control, CHK1 and MK2. |
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| Keywords: | Potency switch CHK1 MK2 Kinase Inhibitor |
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