期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 9, 页码 705-709出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml300074j
关键词
Trk; kinase inhibitors; imidazo[4,5-b]pyridines; purines; cancer
Trk receptor tyrosine kinases have been implicated in cancer and pain. A crystal structure of TrkA with AZ-23 (1a) was obtained, and scaffold hopping resulted in two 5/6-bicyclic series comprising either imidazo[4,5-b]pyridines or purines. Further optimization of these two fusion series led to compounds with subnanomolar potencies against TrkA kinase in cellular assays. Antitumor effects in a TrkA-driven mouse allograft model were demonstrated with compounds 2d and 3a.
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