Pharmaceutical Research Center, School of Chemistry & Chemical Engineering, Southeast University, Nanjing 211189, China.
Bioorg Med Chem. 2012 Feb 15;20(4):1461-7. doi: 10.1016/j.bmc.2011.12.056. Epub 2012 Jan 2.
A number of platinum(II) complexes with ammine or 1R,2R-diaminocyclohexane as carrier ligands and 1-(methoxy-substituted benzyl) azetidine-3,3-dicarboxylate as leaving groups were synthesized and spectrally characterized. Biological evaluation in vitro showed that some of compounds showed positive antitumor activity. In particular, complex 3a, (1R,2R-diaminocyclohexane)[1-(3-methoxylbenzyl) azetidine-3,3-dicarboxylato)-O,O'] platinum(II), possessed a potent antitumor effect comparable to cisplatin and/or oxaliplatin, and very low toxicity in vivo. Preliminary antitumor mechanism of 3a has been investigated by cell apoptosis assays compared with cisplatin and oxaliplatin.
合成了一系列以氨或 1R,2R-二氨基环己烷为载体配体，1-(甲氧基取代苄基)氮杂丁烷-3,3-二羧酸酯为离去基团的铂(II)配合物，并进行了光谱表征。体外生物学评价表明，部分化合物表现出良好的抗肿瘤活性。特别是配合物 3a，（1R,2R-二氨基环己烷）[1-(3-甲氧基苄基)氮杂丁烷-3,3-二羧酸酯基]-O,O'铂(II)，具有与顺铂和/或奥沙利铂相当的强大抗肿瘤作用，且体内毒性很低。与顺铂和奥沙利铂相比，通过细胞凋亡实验初步研究了 3a 的抗肿瘤机制。
