Synthesis of Novel gluco- and galacto-Functionalized Platinum Complexes
Synthesis of Novel gluco- and galacto-Functionalized Platinum Complexes
复制标题
新型葡萄糖和半乳功能化铂配合物的合成
DOI：
10.1002/ejoc.200900691
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发表时间：
2009
影响因子：
2.8
通讯作者：
J. Thiem
中科院分区：
文献类型：
--
作者：
Janina Möker;J. Thiem
顺铂、卡铂、奥沙利铂及其衍生物是世界范围内公认的用于治疗多种肿瘤的细胞抑制剂。这些药物取得了非凡的成功；然而，副作用和肿瘤细胞的原发性或继发性耐药是严重的问题，这促使了新型功能化铂配合物的发展。选择性保护的葡萄糖和半乳糖的单羟基衍生物可以被ω-halo醚化。此外，Finkelstein反应和丙二酸盐合成得到了前体糖缀合物，这些糖缀合物很容易转化为（二胺）铂配合物。对不同肿瘤细胞系的首次试验表明，糖功能化铂复合物具有生物活性。（©Wiley-VCH Verlag GmbH & Co. KGaA，德国Weinheim 69451, 2009）
Cisplatin, carboplatin, oxaliplatin and further derivatives are worldwide established cytostatics for the treatment of a vast range of tumours. These drugs showed extraordinary success; however, side effects and primary or developed secondary resistance of tumour cells represent severe problems, which prompt the development of novel functionalized platinum complexes. Selectively protected monohydroxy derivatives of glucose and galactose could be etherified by ω-halo ethers. Further, Finkelstein reaction and malonate synthesis gave precursor glycoconjugates which were easily transformed into their (diammine)platinum complexes. First tests with different tumour cell lines show biological activity of the gluco-functionalized platinum complex.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)