Quarfloxin

RNA聚合酶I介导的转录抑制剂；与G-四链体DNA结合并抑制核糖体DNAG-四链体与核仁素之间的相互作用；在10µM时诱导A549细胞中的核仁素从核仁错误定位到核质；在5µM时诱导A549和HL-60细胞凋亡；在5mg/kg时降低MDA-MB-231和MiaPaCa-2小鼠异种移植模型中的肿瘤生长。An inhibitor of RNA polymerase I-mediated transcription; binds to G-quadruplex DNA and inhibits the interaction between ribosomal DNA G-quadruplexes and nucleolin; induces nucleolin mislocalization from the nucleoli to the nucleoplasm in A549 cells at 10 µM; induces apoptosis in A549 and HL-60 cells at 5 µM; reduces tumor growth in MDA-MB-231 and MiaPaCa-2 mouse xenograft models at 5 mg/kg.分子式C35H33FN6O3分子量604.7O=C1C2=C3N(C=C1C(NCC[C@@H]4CCCN4C)=O)C5=CC6=CC=CC=C6C=C5OC3=C(N7CC(C8=NC=CN=C8)CC7)C(F)=C2