Nafziger J, Auclair C, Florent J C, Guillosson J J, Monneret C
Laboratoire d'Hématologie, Faculté des Sciences Pharmaceutiques et Biologiques, Paris, France.
Leuk Res. 1991;15(8):709-13. doi: 10.1016/0145-2126(91)90073-3.
The antiproliferative effect of F860191, a new anthracycline with high antitumor activity in L1210 leukemia-inoculated mice, was investigated in vitro on different leukemia cell lines. Comparison of the IC50 value of F860191 with that of daunorubicin and doxorubicin disclosed a superior activity for this drug against the three leukemia cell lines tested. Studies on the mechanism of the antiproliferative activity showed that F860191 induced a G2 + M arrest in the cycle of treated cells. Physicochemical properties of this drug suggested that the high cytotoxic effect of F860191 could be related to its capacity to induce free radicals and to generate DNA breaks through its interaction with topoisomerase II.
F860191是一种新型蒽环类药物，对接种L1210白血病的小鼠具有高抗肿瘤活性。本研究在体外对不同白血病细胞系考察了F860191的抗增殖作用。将F860191与柔红霉素和阿霉素的IC50值进行比较，结果表明该药物对所测试的三种白血病细胞系具有更强的活性。对其抗增殖活性机制的研究表明，F860191可诱导处理细胞周期出现G2+M期阻滞。该药物的物理化学性质表明，F860191的高细胞毒性作用可能与其诱导自由基的能力以及通过与拓扑异构酶II相互作用产生DNA断裂有关。
