Article
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
European journal of medicinal chemistry - 1 Jan 2018
Yang Jiao, Chen Kai, Zhang Guo, Yang Qiu-Yuan, Li Yue-Shan, Huang Shen-Zhen, Wang Yan-Lin, Yang Wei, Jiang Xiao-Juan, Yan Heng-Xiu, Zhu Jing-Qiang, Xiang Rong, Luo You-Fu, Li Wei-Min, Wei Yu-Quan, Li Lin-Li, Yang Sheng-Yong
Abstract excerpt
The RET tyrosine kinase is an important therapeutic target for medullary thyroid cancer (MTC), and drug resistance mutations of RET, particularly V804M and V804L, are a main challenge for the current targeted therapy of MTC based on RET inhibitors. In this investigation, we report the structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine...
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