Design, synthesis and preclinical evaluation of 5-methyl-N 4 -aryl-furo[2,3-d]pyrimidines as single agents with combination chemotherapy potential.
Bioorganic & Medicinal Chemistry Letters(2018)
摘要
•Discovered a new class of single agents for cancer chemotherapy.•Compounds are highly potent inhibitors of tubulin and angiogenesis pathway.•Optimized Ullmann coupling, a key step in the synthesis of target compounds.•Compound 1 showed efficacy in human renal (A498) xenograft model in mice.
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关键词
RTKs,VEGF,VEGFR-2,PDGFR-β,EGFR,ATP,NCI,CA-1,CA-4,PDB,CAM,Pgp
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