Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R

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• 作者：Gangadhar Rao Mathi^a ; ^b ; Chung Hyo Kang^a ; ^c ; Heung Kyoung Lee^a ; Raghavendra Achary^a ; ^b ; Ha-Yeon Lee^a ; ^d ; Joo-Youn Lee^e ; Jae Du Ha^a ; Sunjoo Ahn^a ; ^b ; Chi Hoon Park^a ; ^b ; Chong Ock Lee^a ; Jong Yeon Hwang^a ; ^b ; Chang-Soo Yun^a ; ^b ; Hee Jung Jung^a ; ^b ; Sung Yun Cho^a ; ^b ; Hyoung Rae Kim^a ; ^{hyungrk@krict.re.kr} ; Pilho Kim^a ; ^b ; ^{pkim@krict.re.kr}
• 关键词：Anaplastic lymphoma kinase (ALK) ; Non-small cell lung cancer (NSCLC) ; Ceritinib ; Crizotinib-resistant ; G1202R
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：536-549
• 全文大小：1726 K
• 卷排序：126

文摘

The terminal piperidine in ceritinib was replaced with diverse alkyl amines. Most of the analogs were as active as crizotinib against ALK wild-type and L1196M mutant. Compound 10 has excellent ALK mutant activities including extremely resistant G1202R.