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      Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.

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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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          Author and article information

          Affiliations
          [1 ] AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. Vibha.Oza@astrazeneca.com
          Journal
          Bioorg. Med. Chem. Lett.
          Bioorganic & medicinal chemistry letters
          Elsevier BV
          1464-3405
          0960-894X
          Sep 01 2010
          : 20
          : 17
          S0960-894X(10)00971-6
          10.1016/j.bmcl.2010.07.015
          20673630

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