Antitumor activities and interaction with DNA of oxaliplatin-type platinum complexes with linear or branched alkoxyacetates as leaving groups.
Antitumor activities and interaction with DNA of oxaliplatin-type platinum complexes with linear or branched alkoxyacetates as leaving groups.
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DOI：
10.1016/j.jinorgbio.2011.05.005
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发表时间：
2011-08
影响因子：
3.9
通讯作者：
Runting Yin;S. Gou;Xia Liu;L. Lou
中科院分区：
文献类型：
--
作者：
Runting Yin;S. Gou;Xia Liu;L. Lou
对五种以直链或支链烷氧基羧酸酯为离去基团的反式-1R，2 R-环己烷二氨基螯合铂核的奥沙利铂型铂配合物进行了生物学评价。这些化合物的抗肿瘤活性高于顺铂或奥沙利铂，但体内毒性较低。结果表明，该类化合物的抗肿瘤活性及与DNA的相互作用与离去基团的性质密切相关。在这些配合物中，5a，顺式-（反式-1R，2 R-环己二胺）双（2-叔丁氧乙酸酯）铂（II）表现出最高的抗肿瘤活性和最低的毒性。
Five oxaliplatin-typed platinum complexes containing trans-1R, 2R-diaminocyclohexane chelating platinum cores, characteristic of linear or branched alkoxycarboxylates as leaving groups, were biologically evaluated. These compounds showed higher antitumor activity, lower toxicityin vivothan cisplatin or oxaliplatin. And the results revealed that the antitumor activity and interaction with DNA of these compounds were highly related to the nature of leaving groups. Among these complexes,5a,cis-(trans-1R, 2R-diaminocyclohexane) bis (2-tert-butoxyacetate) platinum(II), showed the highest antitumor activity and the lowest toxicity.