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Synthesis and biological activities of new pyrrolocarbazole-imidazobenzimidazole conjugates
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-05-30 , DOI: 10.1016/j.tetlet.2020.152096 Fabrice Anizon , Francis Giraud , Ekaterina S. Ivanova , Dmitry N. Kaluzhny , Alexander A. Shtil , Federico Cisnetti , Pascale Moreau
中文翻译:
新型吡咯并咔唑-咪唑并苯并咪唑共轭物的合成及生物学活性
更新日期:2020-07-05
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-05-30 , DOI: 10.1016/j.tetlet.2020.152096 Fabrice Anizon , Francis Giraud , Ekaterina S. Ivanova , Dmitry N. Kaluzhny , Alexander A. Shtil , Federico Cisnetti , Pascale Moreau
New pyrrolocarbazole-imidazobenzimidazole conjugates were prepared and evaluated for their inhibitory potencies toward Pim-1 kinase, DNA binding and antiproliferative activities against human tumor cell lines. The results demonstrated that conjugation of pyrrolocarbazole Pim inhibitors with imidazobenzimidazole derivatives could enhance the antiproliferative potency of conjugates compared to the derived compounds.
中文翻译:
新型吡咯并咔唑-咪唑并苯并咪唑共轭物的合成及生物学活性
制备了新的吡咯并咔唑-咪唑并苯并咪唑共轭物,并评估了它们对Pim-1激酶的抑制作用,DNA结合和对人肿瘤细胞系的抗增殖活性。结果表明,与衍生化合物相比,吡咯并咔唑Pim抑制剂与咪唑并苯并咪唑衍生物的缀合可以增强缀合物的抗增殖能力。