文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期，新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
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
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
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 @ 2025

轴向位置含有吲哚基衍生物 5-苯甲氧基吲哚-3-乙酸的铂（IV）前药表现出显著的抗癌活性。

Platinum(IV) Prodrugs Incorporating an Indole-Based Derivative, 5-Benzyloxyindole-3-Acetic Acid in the Axial Position Exhibit Prominent Anticancer Activity.

机构信息

School of Science, Western Sydney University, Sydney, NSW 2751, Australia.

Ingham Institute, Sydney, NSW 2170, Australia.

出版信息

Int J Mol Sci. 2024 Feb 11;25(4):2181. doi: 10.3390/ijms25042181.

DOI:10.3390/ijms25042181
PMID:38396859
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10888562/
Abstract

Kinetically inert platinum(IV) complexes are a chemical strategy to overcome the impediments of standard platinum(II) antineoplastic drugs like cisplatin, oxaliplatin and carboplatin. In this study, we reported the syntheses and structural characterisation of three platinum(IV) complexes that incorporate 5-benzyloxyindole-3-acetic acid, a bioactive ligand that integrates an indole pharmacophore. The purity and chemical structures of the resultant complexes, , and were confirmed via spectroscopic means. The complexes were evaluated for anticancer activity against multiple human cell lines. All complexes proved to be considerably more active than cisplatin, oxaliplatin and carboplatin in most cell lines tested. Remarkably, demonstrated the greatest anticancer activity, displaying GI values between 1.2 and 150 nM. Enhanced production of reactive oxygen species paired with the decline in mitochondrial activity as well as inhibition of histone deacetylase were also demonstrated by the complexes in HT29 colon cells.

摘要

动力学惰性的铂(IV)配合物是克服顺铂、奥沙利铂和卡铂等标准铂(II)抗肿瘤药物障碍的一种化学策略。在这项研究中，我们报告了三种铂(IV)配合物的合成和结构表征，这些配合物包含 5-苄氧基吲哚-3-乙酸，这是一种整合吲哚药效团的生物活性配体。通过光谱手段确认了所得配合物 、 和 的纯度和化学结构。评估了这些配合物对多种人类细胞系的抗癌活性。在大多数测试的细胞系中，所有配合物都被证明比顺铂、奥沙利铂和卡铂活性高得多。值得注意的是，在 HT29 结肠细胞中， 表现出最强的抗癌活性，GI 值在 1.2 到 150 nM 之间。还证明了配合物增强了活性氧的产生，同时降低了线粒体活性，并抑制了组蛋白去乙酰化酶。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/182f1106db60/ijms-25-02181-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/cea94bd19dd2/ijms-25-02181-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/5404ee5f1f89/ijms-25-02181-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/edd56fe28417/ijms-25-02181-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/b51c8f7ebc74/ijms-25-02181-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/eb2c6e8518e1/ijms-25-02181-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/d051ddc5df88/ijms-25-02181-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/e52606e8a798/ijms-25-02181-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/4cd2ed54c4a2/ijms-25-02181-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/5c9b698e870a/ijms-25-02181-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/3ffd4fdb30f3/ijms-25-02181-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/182f1106db60/ijms-25-02181-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/cea94bd19dd2/ijms-25-02181-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/5404ee5f1f89/ijms-25-02181-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/edd56fe28417/ijms-25-02181-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/b51c8f7ebc74/ijms-25-02181-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/eb2c6e8518e1/ijms-25-02181-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/d051ddc5df88/ijms-25-02181-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/e52606e8a798/ijms-25-02181-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/4cd2ed54c4a2/ijms-25-02181-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/5c9b698e870a/ijms-25-02181-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/3ffd4fdb30f3/ijms-25-02181-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0933/10888562/182f1106db60/ijms-25-02181-g011.jpg

相似文献

[1]
Platinum(IV) Prodrugs Incorporating an Indole-Based Derivative, 5-Benzyloxyindole-3-Acetic Acid in the Axial Position Exhibit Prominent Anticancer Activity.

Int J Mol Sci. 2024-2-11

[2]
Potent Chlorambucil-Platinum(IV) Prodrugs.

Int J Mol Sci. 2022-9-9

[3]
Versatile Platinum(IV) Prodrugs of Naproxen and Acemetacin as Chemo-Anti-Inflammatory Agents.

Cancers (Basel). 2023-4-26

[4]
Platinum(II) complexes of imidazophenanthroline-based polypyridine ligands as potential anticancer agents: synthesis, characterization, in vitro cytotoxicity studies and a comparative ab initio, and DFT studies with cisplatin, carboplatin, and oxaliplatin.

J Biol Inorg Chem. 2018-6-14

[5]
Mono- and di-bromo platinum(IV) prodrugs via oxidative bromination: synthesis, characterization, and cytotoxicity.

Dalton Trans. 2015-12-14

[6]
BODI-Pt, a Green-Light-Activatable and Carboplatin-Based Platinum(IV) Anticancer Prodrug with Enhanced Activation and Cytotoxicity.

Inorg Chem. 2020-8-17

[7]
Platinum(IV) Complexes of -1,2-diamino-4-cyclohexene: Prodrugs Affording an Oxaliplatin Analogue that Overcomes Cancer Resistance.

Int J Mol Sci. 2020-3-27

[8]
Thermoresponsive carboplatin-releasing prodrugs.

J Inorg Biochem. 2024-5

[9]
Optimization of axial ligands to promote the photoactivation of BODIPY-conjugated platinum(IV) anticancer prodrugs.

Dalton Trans. 2021-10-12

[10]
Chemotherapeutic Potential of Chlorambucil-Platinum(IV) Prodrugs against Cisplatin-Resistant Colorectal Cancer Cells.

Int J Mol Sci. 2024-7-28

引用本文的文献

[1]
"Non-Classical" Platinum Complexes: A Concise Review.

Int J Mol Sci. 2025-6-28

[2]
Chemotherapeutic Potential of Chlorambucil-Platinum(IV) Prodrugs against Cisplatin-Resistant Colorectal Cancer Cells.

Int J Mol Sci. 2024-7-28

[3]
Anticancer Effect of PtPHEN, Pt5ME, Pt56ME and Their Platinum(IV)-Dihydroxy Derivatives against Triple-Negative Breast Cancer and Cisplatin-Resistant Colorectal Cancer.

Cancers (Basel). 2024-7-15

本文引用的文献

[1]
N-Indolyl diiron vinyliminium complexes exhibit antiproliferative effects in cancer cells associated with disruption of mitochondrial homeostasis, ROS scavenging, and antioxidant activity.

Chem Biol Interact. 2023-11-1

[2]
In the quest for histone deacetylase inhibitors: current trends in the application of multilayered computational methods.

Amino Acids. 2023-12

[3]
The current status in computational exploration of Pt(IV) prodrug activation by reduction.

Phys Chem Chem Phys. 2023-6-15

[4]
Versatile Platinum(IV) Prodrugs of Naproxen and Acemetacin as Chemo-Anti-Inflammatory Agents.

Cancers (Basel). 2023-4-26

[5]
A Review of the Therapeutic Importance of Indole Scaffold in Drug Discovery.

Curr Drug Discov Technol. 2023

[6]
The Challenging Treatment of Cisplatin-Resistant Tumors: State of the Art and Future Perspectives.

Molecules. 2023-4-12

[7]
The impact of histone deacetylase inhibitors on immune cells and implications for cancer therapy.

Cancer Lett. 2023-4-10

[8]
Drug-induced mitochondrial toxicity: Risks of developing glucose handling impairments.

Front Endocrinol (Lausanne). 2023

[9]
Influence of the Fatty Acid Metabolism on the Mode of Action of a Cisplatin(IV) Complex with Phenylbutyrate as Axial Ligands.

Pharmaceutics. 2023-2-16

[10]
Synthesis and Anticancer Evaluation of New Indole-Based Tyrphostin Derivatives and Their (-Cymene)dichloridoruthenium(II) Complexes.

Int J Mol Sci. 2023-1-3

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索