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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Gryshchenko AA,Bdzhola VG,Balanda AO,Briukhovetska NV,Kotey IM,Golub AG,Ruban TP,Lukash LL,Yarmoluk SMdoi
10.1016/j.bmc.2014.12.044subject
Has Abstractpub_date
2015-05-01 00:00:00pages
2287-93issue
9eissn
0968-0896issn
1464-3391pii
S0968-0896(14)00892-Xjournal_volume
23pub_type
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journal_title:Bioorganic & medicinal chemistry
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