Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells
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- 作者：Rita Garamvö ; lgyia ; b ; Judit Dobosb ; Anna Siposb ; Sá ; ndor Borosb ; Eszter Illyé ; sb ; Ferenc Baskab ; Lá ; szló ; Ké ; kesib ; Istvá ; n Szabadkaib ; Csaba Szá ; ntai-Kisb ; Gyö ; rgy Ké ; rib ; c ; Lá ; szló ; Őrfia ; b ; orfi.laszlo@pharma.semmelweis-univ.hu" class="auth_mail" title="E-mail the corresponding author
- 关键词：Imidazo[1 ; 2-a]pyridine ; Imidazo[1 ; 2-a]pyrazine ; Diarylamide ; Diarylurea ; Antiproliferative activity ; A375P ; Melanoma
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：623-643
- 全文大小：978 K
文摘
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A novel series of diarylamide and diarylurea derivatives were synthesized.
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Their antiproliferative activity against A375P human melanoma cell line was tested.
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Compounds 15d, 17e, 18c, 18h, 18i showed IC50 values below 0.06 μM.
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No inhibitory activity on B-Raf(wt) and B-Raf(V600E) kinases could be measured.
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The best compounds were tested on a panel of human lung and colon tumour cell lines.