Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors—Hit to lead exploration |
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| Authors: | Vibha Oza Susan Ashwell Patrick Brassil Jason Breed Chun Deng Jay Ezhuthachan Heather Haye Candice Horn James Janetka Paul Lyne Nicholas Newcombe Ludo Otterbien Martin Pass Jon Read Sian Roswell Mei Su Dorin Toader Dingwei Yu Yan Yu Anna Valentine Xiaolan Zheng |
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| Institution: | 1. AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA;2. AstraZeneca R&D Alderley Park, Cheshire, Macclesfield SK10 4TG, UK |
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| Abstract: | Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ’s) was identified by high throughput screening. The optimization of these hits to provide a lead series is described. |
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