Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors

作者：Packard Garrick K^*; Papa Patrick; Riggs Jennifer R; Erdman Paul; Tehrani Lida; Robinson Dale; Harris Roy; Shevlin Graziella; Perrin Ninkovic Sophie; Hilgraf Robert; McCarrick Margaret A; Tam Tran; Fleming Yuedi; Bai April; Richardson Samantha; Katz Jason; Tang Yang; Leisten Jim; Moghaddam Mehran; Cathers Brian; Zhu Dan; Sakata Steven

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(1): 747-752.

DOI：10.1016/j.bmcl.2011.03.006

• B-Raf inhibitor
• Thieno[2,3-d]pyrimidine
• PDE4 inhibitor

The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described.

• 出版日期2012-1-1