Biomaterials Research Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):413-7. doi: 10.1016/j.bmcl.2009.08.005. Epub 2009 Aug 6.
Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij-k and Iv-w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4'-amide moieties showed the most potent antiproliferative activity against A375.
描述了一系列具有吡咯并[3,2-b]吡啶骨架的新型二芳基脲和酰胺的合成。测试了它们对人黑色素瘤细胞系 A375 和 HS 27 人成纤维细胞系的体外增殖活性，并研究了取代基对吡咯并[3,2-b]吡啶的影响。除间位取代衍生物（Ij-k 和 Iv-w）外，新合成的化合物一般对 A375 的活性优于或与索拉非尼相当。在所有这些衍生物中，具有 5-苄基酰胺取代 4'-酰胺部分的化合物 Ir 和 It 对 A375 表现出最强的增殖抑制活性。
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