Article
Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants.
European journal of medicinal chemistry - 28 Jul 2017
Zhang Haoyang, Wu Wenkui, Feng Chao, Liu Zhaogang, Bai Enhe, Wang Xueyuan, Lei Meng, Cheng Hao, Feng Huayun, Shi Jingmiao, Wang Jia, Zhang Zhao, Jin Tao, Chen Shanshan, Hu Shihe, Zhu Yongqiang
Abstract excerpt
Based upon the modeling binding mode of marketed AZD9291 with T790M, a series of 5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline derivatives were designed and synthesized with the purpose to overcome the drug resistance resulted from T790M/L858R double mutations. The most potent compound 8 showed excellent enzyme inhibitory activities and selectivity with sub nanomolar IC50 values for both the single L858R and double...
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