Discovery of a Novel, Selective and Irreversible Inhibitor (Abivertinib) of Mutated EGFR and T790M-induced Resistance for the Treatment of NSCLC

• Main Authors: Long Mao (Author), Wei Tang (Author), Xiaoying Zhang (Author), Jia Liu (Author), Yile Chen (Author), Yuning Hua (Author), Bojie Weng (Author), Xiaopeng Mo (Author), Yimei Bao (Author), Li Teng (Author), Lijun Xu (Author), Yuren Zhang (Author), Jian Wu (Author), Guanglin Zhou (Author), Bin Liang (Author), Changxu Xu (Author), Biao Xi (Author), Li Zhao (Author), Rongda Xu (Author), Che Fang (Author), Wanhong Xu (Author), Xiaobo Wang (Author), Xiao Xu (Author)
• Format: Book
• Published: Elsevier, 2020-06-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Three chemical series of heterocyclic small molecules were designed and synthesized as the 3rd generation EGFR inhibitors. Detailed structure-activity relationship (SAR) studies and lead optimization (from 1a to 4d) were descripted. With the support of molecular modeling and evaluation through bioch...