期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 5, 页码 1315-1319出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.071
关键词
MEK; Kinase; SBDD; Allosteric; Pyridopyrimidinedione; Oncology
资金
- Office of Science, Office of Basic Energy Sciences, Materials Sciences Division, of the U. S. Department of Energy (DOE) at Lawrence Berkeley National Laboratory [DE-AC02-05CH11231]
A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for cancer treatment. (C) 2011 Elsevier Ltd. All rights reserved.
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