Department of Chemistry, University of Nevada, Las Vegas, 4505 Maryland Parkway, Box 454003, Las Vegas, NV 89154-4003, United States.
Bioorg Med Chem. 2010 Feb;18(3):1163-70. doi: 10.1016/j.bmc.2009.12.047. Epub 2010 Jan 4.
The synthesis and characterization of dichloro(4,4'-bis[methoxy]-2,2'-bipyridine)platinum (1) and dichloro(4,4'-bis[3-methoxy-n-propyl]-2,2'-bipyridine)platinum (2) are described. As analogues to CDDP, these 4,4'-disubstituted 2,2'-bipyridine complexes exhibit decreased EC(50) values of 10-100 times in cancer cell lines of the lung, prostate, and melanoma with several combinations of complex and cell line less than 10 microM. Flow cytometry data indicate 'blocks' of MDA-MD-435 cycle by 1 (G2/M) and 2 (S). Observed cell survival trends in the presence of 1, 2 under ionizing radiation mimic those of CDDP. Preliminary structure activity relationships are discussed for the 4,4'-substitutions made on the bipyridine ring.
二氯（4,4'-双[甲氧基]-2,2'-联吡啶）铂（1）和二氯（4,4'-双[3-甲氧基-n-丙基]-2,2'-联吡啶）铂（2）的合成和表征。作为 CDDP 的类似物，这些 4,4'-取代的 2,2'-联吡啶配合物在肺癌、前列腺癌和黑色素瘤的癌细胞系中的 EC(50) 值降低了 10-100 倍，其中一些配合物和细胞系的浓度低于 10 microM。流式细胞术数据表明 1（G2/M）和 2（S）阻断 MDA-MD-435 周期。在存在 1 和 2 的情况下观察到的细胞存活趋势与 CDDP 的相似。初步的结构活性关系讨论了在联吡啶环上进行的 4,4'-取代。
