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Bioorg Med Chem ; 23(9): 2287-93, 2015 May 01.
Article in English | MEDLINE | ID: mdl-25817240

ABSTRACT

Fibroblast grow factor receptor 1 (FGFR1) is an important anti-cancer target that plays crucial role in oncogenesis and oncogenic angiogenesis. The structure-activity relationship (SAR) of N-phenylthieno[2,3-d]pyrimidin-4-amines was investigated. Binding of active compounds with FGFR1 kinase was analyzed by molecular modeling studies. Selected active thieno[2,3-d]pyrimidines were tested for selectivity and antiproliferative activity. The most active compounds, 3-({6-phenylthieno[2,3-d]pyrimidin-4-yl}amino)phenol and 3-({5-phenylthieno[2,3-d]pyrimidin-4-yl}amino)phenol have IC50 0.16 and 0.18 µM, respectively. The results presented here may help to identify new thienopyrimidines with optimized cell growth inhibitory activity which may be further used as anticancer agents.


Subject(s)
Drug Design , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/pharmacology , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Receptor, Fibroblast Growth Factor, Type 1/antagonists & inhibitors , Thiophenes/chemical synthesis , Thiophenes/pharmacology , Cell Line, Tumor , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Humans , Molecular Docking Simulation , Molecular Structure , Protein Kinase Inhibitors/chemistry , Pyrimidines/chemistry , Receptor, Fibroblast Growth Factor, Type 1/metabolism , Structure-Activity Relationship , Thiophenes/chemistry
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