ALK inhibitors of bis-ortho-alkoxy-para-piperazinesubstitutedpyrimidines and -triazines for cancer treatment

Syntheses of various bis-ortho-alkoxy-parapiperazineanilino-pyrimidines and -triazines of KRCA-0008 analogs are described and their structure–activityrelationshipto anaplastic lymphoma kinase (ALK) is discussed. 5-trifluoromethyl-2,4-pyrimidine analog (2) seemsto be most potent in both biochemical a...

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Published inArchives of pharmacal research pp. 1130 - 1138
Main Authors 이현지, Muhammad Latif, 조현정, Imran Ali, 이흥경, 양은혜, 윤정인, 채정학, 정재경, 김형래, Chong-OckLee, 박지훈, LEEKWANGHO
Format Journal Article
LanguageEnglish
Published 대한약학회 01.09.2014
Subjects
약학
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ISSN0253-6269
1976-3786

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Summary:Syntheses of various bis-ortho-alkoxy-parapiperazineanilino-pyrimidines and -triazines of KRCA-0008 analogs are described and their structure–activityrelationshipto anaplastic lymphoma kinase (ALK) is discussed. 5-trifluoromethyl-2,4-pyrimidine analog (2) seemsto be most potent in both biochemical and cellular assay inthis study, however it shows inferior mice xenograftactivity to Crizotinib presumably due to its sub-optimal PKparameters. 4,6-disubstituted pyrimidine and 2,4-disubstitutedtriazine derivatives of KRCA-0008 are less potent orinactive to ALK wt., and this observation is explained withtheir molecular modeling compared to KRCA-0008. KCI Citation Count: 13
Bibliography:G704-000010.2014.37.9.014
ISSN:0253-6269
1976-3786