• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

新型双（羧基）二氯二乙胺合铂（IV）配合物的合成与表征，其细胞毒性高于顺铂。

Synthesis and characterization of novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes with higher cytotoxicity than cisplatin.

机构信息

University of Vienna, Institute of Inorganic Chemistry, Währinger Strasse 42, A-1090 Vienna, Austria.

出版信息

Eur J Med Chem. 2011 Nov;46(11):5456-64. doi: 10.1016/j.ejmech.2011.09.006. Epub 2011 Sep 8.

DOI:10.1016/j.ejmech.2011.09.006
PMID:21940073
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3206992/
Abstract

A series of six novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes was synthesized and characterized in detail by elemental analysis, FT-IR, ESI-MS, HPLC, multinuclear ((1)H, (13)C, (15)N, (195)Pt) NMR spectroscopy and in one case by X-ray diffraction. Cytotoxic properties of the complexes were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1 and SK-OV-3), colon carcinoma (SW480) and non-small cell lung cancer (A549) by means of the MTT colorimetrical assay. In addition, their octanol/water partition coefficients (log P values) were determined. Remarkably the most active (and also most lipophilic) compounds, having 4-propyloxy-4-oxobutanoato and 4-(2-propyloxy)-4-oxobutanoato axial ligands, showed IC(50) values down to the low nanomolar range.

摘要

合成并详细表征了一系列六种新型双（羧酸根）二氯二（乙胺）合铂（IV）配合物，通过元素分析、FT-IR、ESI-MS、HPLC、多核（^1H、^13C、^15N、^195Pt）NMR 光谱和 X 射线衍射进行了表征。通过 MTT 比色法在源自卵巢癌（CH1 和 SK-OV-3）、结肠癌（SW480）和非小细胞肺癌（A549）的四种人肿瘤细胞系中评估了配合物的细胞毒性。此外，还测定了它们的辛醇/水分配系数（log P 值）。值得注意的是，最具活性（也是最亲脂性）的化合物具有 4-丙氧基-4-氧代丁酸酯和 4-（2-丙氧基）-4-氧代丁酸酯轴向配体，其 IC（50）值低至纳摩尔范围。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/a6d4124577da/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/48a781b84a3a/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/31ab1f909fe1/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/c9b7ead6ae03/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/d2c1fcdfb2ca/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/984945449dd6/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/5119f3b59ccb/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/edc3d9343176/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/a6d4124577da/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/48a781b84a3a/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/31ab1f909fe1/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/c9b7ead6ae03/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/d2c1fcdfb2ca/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/984945449dd6/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/5119f3b59ccb/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/edc3d9343176/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ede/3206992/a6d4124577da/gr7.jpg

相似文献

1
Synthesis and characterization of novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes with higher cytotoxicity than cisplatin.新型双（羧基）二氯二乙胺合铂（IV）配合物的合成与表征，其细胞毒性高于顺铂。
Eur J Med Chem. 2011 Nov;46(11):5456-64. doi: 10.1016/j.ejmech.2011.09.006. Epub 2011 Sep 8.
2
Bis- and Tetrakis(carboxylato)platinum(IV) complexes with mixed axial ligands - synthesis, characterization, and cytotoxicity.含混合轴向配体的双（羧基）和四（羧基）铂（IV）配合物——合成、表征及细胞毒性
Chem Biodivers. 2015 Apr;12(4):559-74. doi: 10.1002/cbdv.201400291.
3
Novel bis(carboxylato)dichlorido(ethane-1,2-diamine)platinum(IV) complexes with exceptionally high cytotoxicity.具有极高细胞毒性的新型双（羧基）二氯（乙二胺）铂（IV）配合物。
J Inorg Biochem. 2008 Dec;102(12):2072-7. doi: 10.1016/j.jinorgbio.2008.07.006. Epub 2008 Jul 23.
4
Tetracarboxylatoplatinum(IV) complexes featuring monodentate leaving groups - A rational approach toward exploiting the platinum(IV) prodrug strategy.具有单齿离去基团的四羧基铂（IV）配合物——开发铂（IV）前药策略的合理方法。
J Inorg Biochem. 2015 Dec;153:259-271. doi: 10.1016/j.jinorgbio.2015.08.018. Epub 2015 Aug 28.
5
Diamminetetrakis(carboxylato)platinum(IV) complexes--synthesis, characterization, and cytotoxicity.二氨四(羧酸根)合铂(IV)配合物的合成、表征及细胞毒性。
Chem Biodivers. 2012 Sep;9(9):1840-8. doi: 10.1002/cbdv.201200019.
6
Mono-carboxylated diaminedichloridoplatinum(IV) complexes--selective synthesis, characterization, and cytotoxicity.单羧基二胺二氯合铂（IV）配合物的选择性合成、表征和细胞毒性。
Dalton Trans. 2011 Aug 28;40(32):8187-92. doi: 10.1039/c1dt10301f. Epub 2011 Jul 11.
7
The synthesis, spectroscopic, X-ray characterization and in vitro cytotoxic testing results of activity of five new trans-platinum(IV) complexes with functionalized pyridines.五种含功能化吡啶的新型反式铂（IV）配合物的合成、光谱、X射线表征及体外细胞毒性活性测试结果
Eur J Med Chem. 2012 Sep;55:214-9. doi: 10.1016/j.ejmech.2012.07.019. Epub 2012 Jul 22.
8
Novel endothall-containing platinum(IV) complexes: synthesis, characterization, and cytotoxic activity.新型含烯草酮的铂（IV）配合物：合成、表征及细胞毒性活性。
Chem Biodivers. 2008 Oct;5(10):2160-2170. doi: 10.1002/cbdv.200890197.
9
Novel cis- and trans-configured bis(oxime)platinum(II) complexes: synthesis, characterization, and cytotoxic activity.新型顺式和反式双（肟）铂（II）配合物的合成、表征及细胞毒性活性。
Inorg Chem. 2010 Jun 21;49(12):5669-78. doi: 10.1021/ic100584b.
10
Novel di- and tetracarboxylatoplatinum(IV) complexes. Synthesis, characterization, cytotoxic activity, and DNA platination.新型二羧酸和四羧酸铂（IV）配合物。合成、表征、细胞毒性活性及DNA铂化作用。
J Med Chem. 2007 Dec 27;50(26):6692-9. doi: 10.1021/jm070897b. Epub 2007 Nov 22.

引用本文的文献

1
Development of Cytotoxic GW7604-Zeise's Salt Conjugates as Multitarget Compounds with Selectivity for Estrogen Receptor- Positive Tumor Cells.开发细胞毒性 GW7604-Zeise 的盐缀合物作为多靶点化合物，对雌激素受体阳性肿瘤细胞具有选择性。
J Med Chem. 2024 Mar 28;67(6):4870-4888. doi: 10.1021/acs.jmedchem.3c02454. Epub 2024 Mar 13.
2
Pyrenebutyrate Pt(IV) Complexes with Nanomolar Anticancer Activity.具有纳摩尔抗癌活性的丁酸芘铂（IV）配合物
Pharmaceutics. 2023 Sep 13;15(9):2310. doi: 10.3390/pharmaceutics15092310.
3
Platinum(IV)-Loaded Degraded Glycol Chitosan as Efficient Platinum(IV) Drug Delivery Platform.

本文引用的文献

1
Tuning of lipophilicity and cytotoxic potency by structural variation of anticancer platinum(IV) complexes.通过抗癌铂(IV)配合物的结构变化来调节亲脂性和细胞毒性效力。
J Inorg Biochem. 2011 Jan;105(1):46-51. doi: 10.1016/j.jinorgbio.2010.09.006. Epub 2010 Oct 1.
2
The status of platinum anticancer drugs in the clinic and in clinical trials.铂类抗癌药物在临床和临床试验中的地位。
Dalton Trans. 2010 Sep 21;39(35):8113-27. doi: 10.1039/c0dt00292e. Epub 2010 Jun 30.
3
The first example of MEEKC-ICP-MS coupling and its application for the analysis of anticancer platinum complexes.
负载铂（IV）的降解壳聚糖二醇作为高效的铂（IV）药物递送平台。
Pharmaceutics. 2023 Mar 24;15(4):1050. doi: 10.3390/pharmaceutics15041050.
4
Impact of Hydrophobic Chains in Five-Coordinate Glucoconjugate Pt(II) Anticancer Agents.五配位葡糖基铂(II)抗癌配合物中疏水性链的影响。
Int J Mol Sci. 2023 Jan 25;24(3):2369. doi: 10.3390/ijms24032369.
5
Synthesis, crystal structure, cytotoxicity and action mechanism of a Rh(iii) complex with 8-hydroxy-2-methylquinoline as a ligand.以8-羟基-2-甲基喹啉为配体的铑(iii)配合物的合成、晶体结构、细胞毒性及作用机制
Medchemcomm. 2016 Oct 25;8(1):184-190. doi: 10.1039/c6md00462h. eCollection 2017 Jan 1.
6
Multi-scale imaging of anticancer platinum(iv) compounds in murine tumor and kidney.抗癌铂（IV）化合物在小鼠肿瘤和肾脏中的多尺度成像
Chem Sci. 2016 May 1;7(5):3052-3061. doi: 10.1039/c5sc04383b. Epub 2016 Feb 3.
7
The impact of whole human blood on the kinetic inertness of platinum(iv) prodrugs - an HPLC-ICP-MS study.全血对顺铂前药动力学惰性的影响 - HPLC-ICP-MS 研究。
Dalton Trans. 2018 Apr 17;47(15):5252-5258. doi: 10.1039/c7dt04537a.
8
Activation of Platinum(IV) Prodrugs By Motexafin Gadolinium as a Redox Mediator.莫替沙芬钆激活铂（IV）前药作为一种氧化还原介体。
Angew Chem Int Ed Engl. 2016 Oct 4;55(41):12626-31. doi: 10.1002/anie.201604236. Epub 2016 Jul 5.
9
From Synthesis to Biological Impact of Pd (II) Complexes: Synthesis, Characterization, and Antimicrobial and Scavenging Activity.钯（II）配合物从合成到生物影响：合成、表征以及抗菌和清除活性
Biochem Res Int. 2016;2016:4359375. doi: 10.1155/2016/4359375. Epub 2016 Mar 16.
10
Tumor microenvironment in focus: LA-ICP-MS bioimaging of a preclinical tumor model upon treatment with platinum(IV)-based anticancer agents.聚焦肿瘤微环境：基于铂（IV）的抗癌药物治疗后临床前肿瘤模型的激光烧蚀电感耦合等离子体质谱生物成像
Metallomics. 2015 Aug;7(8):1256-64. doi: 10.1039/c5mt00028a. Epub 2015 Apr 9.
微乳液电动色谱-电感耦合等离子体质谱联用及其在抗癌铂配合物分析中的应用。
Electrophoresis. 2010 Apr;31(7):1144-1150. doi: 10.1002/elps.200900522.
4
Novel endothall-containing platinum(IV) complexes: synthesis, characterization, and cytotoxic activity.新型含烯草酮的铂（IV）配合物：合成、表征及细胞毒性活性。
Chem Biodivers. 2008 Oct;5(10):2160-2170. doi: 10.1002/cbdv.200890197.
5
Novel bis(carboxylato)dichlorido(ethane-1,2-diamine)platinum(IV) complexes with exceptionally high cytotoxicity.具有极高细胞毒性的新型双（羧基）二氯（乙二胺）铂（IV）配合物。
J Inorg Biochem. 2008 Dec;102(12):2072-7. doi: 10.1016/j.jinorgbio.2008.07.006. Epub 2008 Jul 23.
6
Calculation of lipophilicity for Pt(II) complexes: experimental comparison of several methods.铂（II）配合物亲脂性的计算：几种方法的实验比较
J Inorg Biochem. 2008 Jul;102(7):1424-37. doi: 10.1016/j.jinorgbio.2007.12.029. Epub 2008 Jan 8.
7
Recent Developments in the Field of Anticancer Platinum Complexes.抗癌铂配合物领域的最新进展
Recent Pat Anticancer Drug Discov. 2006 Jun;1(2):285-95. doi: 10.2174/157489206777442287.
8
A short history of SHELX.SHELX简史。
Acta Crystallogr A. 2008 Jan;64(Pt 1):112-22. doi: 10.1107/S0108767307043930. Epub 2007 Dec 21.
9
Novel di- and tetracarboxylatoplatinum(IV) complexes. Synthesis, characterization, cytotoxic activity, and DNA platination.新型二羧酸和四羧酸铂（IV）配合物。合成、表征、细胞毒性活性及DNA铂化作用。
J Med Chem. 2007 Dec 27;50(26):6692-9. doi: 10.1021/jm070897b. Epub 2007 Nov 22.
10
Basis for design and development of platinum(IV) anticancer complexes.铂（IV）抗癌配合物的设计与开发基础。
J Med Chem. 2007 Jul 26;50(15):3403-11. doi: 10.1021/jm070280u. Epub 2007 Jun 28.