某些苯并咪唑-4,7-二酮作为生物还原抗癌剂的合成及细胞毒性评估
Synthesis and cytotoxicity evaluation of some benzimidazole-4,7-diones as bioreductive anticancer agents.
作者信息
Gellis Armand, Kovacic Hervé, Boufatah Narimène, Vanelle Patrice
机构信息
Laboratoire de Chimie Organique Pharmaceutique, UMR CNRS 6517, Université de la Méditerranée, Faculté de Pharmacie, 27 Boulevard Jean Moulin, 13385 Marseille Cedex 05, France.
出版信息
Eur J Med Chem. 2008 Sep;43(9):1858-64. doi: 10.1016/j.ejmech.2007.11.020. Epub 2007 Dec 15.
New benzimidazole-4,7-diones substituted at 2-position were synthesized via a microwave-assisted reaction using 2-chloromethyl-1,5,6-trimethyl-1H-benzimidazole-4,7-dione 5b as a key intermediate compound. Their cytotoxicity has been evaluated on colon, breast and lung cancer cell lines. The dimer 17 was shown to possess excellent cytotoxicity comparable to that of mitomycin C.
通过微波辅助反应，以2-氯甲基-1,5,6-三甲基-1H-苯并咪唑-4,7-二酮5b作为关键中间体化合物，合成了在2-位被取代的新型苯并咪唑-4,7-二酮。已对其在结肠、乳腺和肺癌细胞系上的细胞毒性进行了评估。二聚体17显示出与丝裂霉素C相当的优异细胞毒性。
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