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 ; lgyi^a ; ^b ; Judit Dobos^b ; Anna Sipos^b ; Sá ; ndor Boros^b ; Eszter Illy&eacute ; s^b ; Ferenc Baska^b ; Lá ; szló ; K&eacute ; kesi^b ; Istvá ; n Szabadkai^b ; Csaba Szá ; ntai-Kis^b ; Gyö ; rgy K&eacute ; ri^b ; ^c ; Lá ; szló ; Őrfi^a ; ^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

<dl class="listitem" id="list_ulist0010"><dt class="label">•dt><dd>

d="p0010">A novel series of diarylamide and diarylurea derivatives were synthesized.

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d="p0015">Their antiproliferative activity against A375P human melanoma cell line was tested.

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d="p0020">Compounds dFont">15d, dFont">17e, dFont">18c, dFont">18h, dFont">18i showed IC₅₀ values below 0.06 μM.

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d="p0025">No inhibitory activity on B-Raf(wt) and B-Raf(V600E) kinases could be measured.

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d="p0030">The best compounds were tested on a panel of human lung and colon tumour cell lines.

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