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2,3-取代吲哚类化合物对凋亡抵抗性癌细胞的抗增殖活性。

Antiproliferative activity of 2,3-disubstituted indoles toward apoptosis-resistant cancers cells.

机构信息

Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA.

出版信息

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3277-82. doi: 10.1016/j.bmcl.2013.03.110. Epub 2013 Apr 8.

DOI:10.1016/j.bmcl.2013.03.110
PMID:23622980
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3915534/
Abstract

Many types of cancer, including glioma, melanoma, NSCLC, among others, are resistant to apoptosis induction and poorly responsive to current therapies with propaptotic agents. We describe a series of 2,3-disubstituted indoles, which display cytostatic rather than cytotoxic effects in cancer cells, and serve as a new chemical scaffold to develop anticancer agents capable of combating apoptosis-resistant cancers associated with dismal prognoses.

摘要

许多类型的癌症,包括神经胶质瘤、黑色素瘤、非小细胞肺癌等,对凋亡诱导具有抗性,并且对当前使用促凋亡剂的治疗反应不佳。我们描述了一系列 2,3-取代的吲哚,它们在癌细胞中表现出细胞生长抑制而非细胞毒性作用,并作为开发能够对抗与预后不良相关的抗凋亡癌症的抗癌药物的新化学支架。

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引用本文的文献

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Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines.倍半萜多香树醛的维蒂希衍生化反应可生成对耐药癌细胞具有活性且能够使伯胺发生吡咯化反应的细胞生长抑制剂。
Eur J Med Chem. 2015 Oct 20;103:226-37. doi: 10.1016/j.ejmech.2015.08.047. Epub 2015 Aug 29.
2
Activity of 2-aryl-2-(3-indolyl)acetohydroxamates against drug-resistant cancer cells.2-芳基-2-(3-吲哚基)乙酰氧肟酸对耐药癌细胞的活性。
J Med Chem. 2015 Mar 12;58(5):2206-20. doi: 10.1021/jm501518y. Epub 2015 Feb 20.

本文引用的文献

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Amaryllidaceae alkaloids belonging to different structural subgroups display activity against apoptosis-resistant cancer cells.石蒜科生物碱属于不同结构亚组,对抗细胞凋亡的癌细胞具有活性。
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Natural polyphenols that display anticancer properties through inhibition of kinase activity.具有抑制激酶活性的抗癌特性的天然多酚类化合物。
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Lycorine, the main phenanthridine Amaryllidaceae alkaloid, exhibits significant antitumor activity in cancer cells that display resistance to proapoptotic stimuli: an investigation of structure-activity relationship and mechanistic insight.石蒜碱是石蒜科主要的菲啶生物碱,在对促凋亡刺激具有抗性的癌细胞中表现出显著的抗肿瘤活性:结构-活性关系及作用机制研究
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