Wang Lianhong, Gou Shaohua, Chen Yongjiang, Liu Yun
State Key Laboratory of Coordination Chemistry, Nanjing University, Nanjing 210093, China.
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3417-22. doi: 10.1016/j.bmcl.2005.05.025.
Eight new camphorato platinum complexes have been synthesized and evaluated for their in vitro cytotoxicity against HL-60 human leukemia, 3AO human ovarian carcinoma, BEL-7402 human hepatocarcinoma, and A549 human lung carcinoma cell lines. Most complexes showed good cytotoxic activity against the above-selected cell lines. Among the complexes, two compounds were assayed for their in vivo antitumor activity against LS-174T human colon carcinoma cells implanted in mice. One complex exhibited not only higher in vivo antitumor activity, but also less toxicity than oxaliplatin when it was administered intravenously at a dose of 6 mg/kg three times.
已合成了八种新的樟脑酸铂配合物,并评估了它们对HL-60人白血病细胞系、3AO人卵巢癌细胞系、BEL-7402人肝癌细胞系和A549人肺癌细胞系的体外细胞毒性。大多数配合物对上述所选细胞系表现出良好的细胞毒性活性。在这些配合物中,对两种化合物进行了针对植入小鼠体内的LS-174T人结肠癌细胞的体内抗肿瘤活性测定。当以6mg/kg的剂量静脉注射三次时,一种配合物不仅表现出更高的体内抗肿瘤活性,而且毒性比奥沙利铂更小。