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Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors |
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| Authors: | Ni Yike Gopalsamy Ariamala Cole Derek Hu Yonghan Denny Rajiah Ipek Manus Liu Julie Lee Julie Hall J Perry Luong Michael Telliez Jean-Baptiste Lin Lih-Ling |
| Institution: | Medicinal Chemistry, Pfizer, 200 Cambridge Park Drive, Cambridge, MA 02140, USA. yike.ni@pfizer.com |
| Abstract: | We report here the synthesis and SAR of a new series of thieno3,2-d]pyrimidines as potent Tpl2 kinase inhibitors. The proposed binding mode suggests the potential flipped binding mode depending on the substitution. Biacore studies show evidence of binding of these molecules to the protein kinase. The kinome inhibition profile of these molecules suggests good selectivity. |
| Keywords: | Tpl2 kinase Thieno[3 2-d]pyrimidine |
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