Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 4, Pages 304-308Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml400373j
Keywords
C1-Substituted-N3-benzazepine; c-Met/ALK dual inhibitor; structure repurposing; 2,4-diarylaminopyrimidine analogues
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Funding
- Chinese NSF [81125021, 81373277, 81102461, 91229205]
- National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program' China [2012ZX09103-101-035, 2012ZX09301001-007, 2012ZX09301001-001]
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By repurposing a typical dopamine D-1/D-5 receptor agonist motif, C1-substituted-N3-benzazepine or benzazecine, into the classical RTK inhibitor 2,4-diaminopyrimidine skeleton, a series of new 2,4-diarylaminopyrimidine analogues (DAAPalogues) were developed. Compounds 7 and 8a were identified possessing high potency against both c-Met and ALK kinases. Compound 8a displayed appreciable antitumor efficacy at the dose of 1 mg/kg in the ALK-driven BF3/EML4-ALK xenograft mice model.
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