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来自樟脑酸(一种中药衍生物)与铂部分创新组合的潜在新型抗肿瘤药物。

Potential new antitumor agents from an innovative combination of camphorato, a ramification of traditional Chinese medicine, with a platinum moiety.

作者信息

Wang Lianhong, Gou Shaohua, Chen Yongjiang, Liu Yun

机构信息

State Key Laboratory of Coordination Chemistry, Nanjing University, Nanjing 210093, China.

出版信息

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3417-22. doi: 10.1016/j.bmcl.2005.05.025.

Abstract

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.

摘要

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。

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