Substituted benzimidazole compound and application thereof

The invention relates to the field of medicine, in particular to a substituted benzimidazole compound and application thereof.The substituted benzimidazole compound has remarkable inhibitory activity to FLT3 kinase, the IC50 value of the compound to the FLT3 kinase reaches the highest single-digit n...

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Hauptverfasser: XUE GUIMIN, ZHAO ZHENZHU, GONG JIANHONG, WU YA, ZHANG ZHIQIANG, CHEN HUI, ZHANG FEI, ZHI YANLE, FENG WEISHENG, LI XIAOKUN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the field of medicine, in particular to a substituted benzimidazole compound and application thereof.The substituted benzimidazole compound has remarkable inhibitory activity to FLT3 kinase, the IC50 value of the compound to the FLT3 kinase reaches the highest single-digit nanomole level, meanwhile, the compound also shows remarkable anti-proliferative activity to a leukemia cell strain MV4-11, and the compound can be used for preparing a medicine for treating leukemia. The compound can be used as a novel and powerful FLT3 inhibitor, and lays a foundation for research and development of novel antitumor drugs targeting FLT3. 本发明涉及医药领域,具体涉及取代的苯并咪唑类化合物及其应用,本发明的化合物对FLT3激酶具有显著的抑制活性,对FLT3激酶的IC50值最高达到了个位数纳摩尔级别,同时其对白血病细胞株MV4-11也表现出了显著的抗增殖活性,该类化合物可作为新型强效的FLT3抑制剂,为靶向FLT3的新型抗肿瘤药物的研发奠定了基础。