Mononuclear tetraamineplatinum(II) complexes: Synthesis, anticancer activity, DNA binding, and cellular uptake
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作者:
Robillard, Marc S.
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Leiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, NetherlandsLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Robillard, Marc S.
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Jansen, Bart A. J.
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Leiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, NetherlandsLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Jansen, Bart A. J.
[1
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Lochner, Martin
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Organisch-chemisches Institut, Universität Zürich, Winterthurerstrasse 190, CH-8057 Zürich, SwitzerlandLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Lochner, Martin
[2
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Geneste, Hervé
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Organisch-chemisches Institut, Universität Zürich, Winterthurerstrasse 190, CH-8057 Zürich, SwitzerlandLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Geneste, Hervé
[2
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Li, Yi
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Organisch-chemisches Institut, Universität Zürich, Winterthurerstrasse 190, CH-8057 Zürich, SwitzerlandLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Li, Yi
[2
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Brouwer, Jaap
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Leiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, NetherlandsLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Brouwer, Jaap
[1
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Hesse, Manfred
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Organisch-chemisches Institut, Universität Zürich, Winterthurerstrasse 190, CH-8057 Zürich, SwitzerlandLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Hesse, Manfred
[2
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Reedijk, Jan
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Leiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, NetherlandsLeiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
Reedijk, Jan
[1
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[1] Leiden Institute of Chemistry, P.O. Box 9502, NL-2300 RA Leiden, Netherlands
[2] Organisch-chemisches Institut, Universität Zürich, Winterthurerstrasse 190, CH-8057 Zürich, Switzerland
The synthesis of three bis[(tert-butoxy)carbonyl]-protected (tetramine)dichloroplatinum complexes 2a-c of formula cis-[PtCl2(LL)] and of their cationic deprotected analogs 3a-c and their evaluation with respect to in vitro cytotoxicity, intramolecular stability, DNA binding, and cellular uptake is reported. The synthesis comprises the complexation of K2[PtCl4] with di-N-protected tetramines 1a-c to give 2a-c and subsequent acidolysis, yielding 3a-c. The cytotoxicity of the complexes is in direct relation to the length of the polyamine. Complexes 3a-c display a significant higher affinity for CT DNA as well as for cellular DNA in A2780 cells than cisplatin.
机构:
Guangdong Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Guangzhou 510006, Guangdong, Peoples R ChinaGuangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China
Huang, Hong-Liang
Li, Zheng-Zheng
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Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R ChinaGuangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China
Li, Zheng-Zheng
Liang, Zhen-Hua
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Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R ChinaGuangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China
Liang, Zhen-Hua
Yao, Jun-Hua
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机构:
Sun Yat Sen Univ, Instrumentat Anal & Res Ctr, Guangzhou 510275, Guangdong, Peoples R ChinaGuangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China
Yao, Jun-Hua
Liu, Yun-Jun
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机构:
Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China
Guangdong Pharmaceut Univ, Sch Chem & Chem Engn, Guangzhou 510006, Guangdong, Peoples R ChinaGuangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China