Amonafide

DNA插入拓扑异构酶II毒物；在无细胞测定中，浓度为100µM时可减少动基体DNA微环的形成，但不会诱导超螺旋DNA松弛；抑制11种人类癌细胞系（包括白血病、胃癌、乳腺癌和肺癌细胞(GI50s=1-10µM)）的生长；浓度为2.5-10µM时，可分别诱导AGS胃癌和Huh7肝癌细胞在G2/M期细胞周期停滞和凋亡；在5mg/kg时，可减缓小鼠H22肝癌模型中的原发性肿瘤生长并降低肺转移。A DNA-intercalating topoisomerase II poison; reduces the formation of kinetoplast DNA minicircles in a cell-free assay at 100 µM, but does not induce relaxation of supercoiled DNA; inhibits growth in a panel of 11 human cancer cell lines including leukemia, gastric, breast, and lung cancer cells (GI50s = 1-10 µM); induces cell cycle arrest at the G2/M phase and apoptosis in AGS gastric and Huh7 hepatoma cancer cells, respectively, from 2.5-10 µM; reduces primary tumor growth and decreases pulmonary metastasis in a murine H22 hepatoma model at 5 mg/kg.分子式C16H17N3O2分子量283.3O=C1C2=C3C(C(N1CCN(C)C)=O)=CC(N)=CC3=CC=C2