Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs

Carboline consists of a pyridine ring fused with an indole skeleton, and it serves as a potential drug scaffold. Depending on the relative position of the pyridine N to the indole N, carbolines can be categorized into α-, β-, γ-, and δ-subfamilies. They have diverse pharmacological activities, such...

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Main Authors: Jingliang Cui, Wanru Gao, Ziwei Liu, Shuang Cao, Sihui Long
Format: Article
Language:English
Published: Elsevier 2024-12-01
Series:European Journal of Medicinal Chemistry Reports
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Online Access:http://www.sciencedirect.com/science/article/pii/S2772417424000931
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author Jingliang Cui
Wanru Gao
Ziwei Liu
Shuang Cao
Sihui Long
author_facet Jingliang Cui
Wanru Gao
Ziwei Liu
Shuang Cao
Sihui Long
author_sort Jingliang Cui
collection DOAJ
description Carboline consists of a pyridine ring fused with an indole skeleton, and it serves as a potential drug scaffold. Depending on the relative position of the pyridine N to the indole N, carbolines can be categorized into α-, β-, γ-, and δ-subfamilies. They have diverse pharmacological activities, such as anticancer, antimalaria, antibacterial, antifungal, anti-Alzheimer's disease, etc. Among them, β-carbolines are the most widely studied and are also well reviewed. Herein, we review the anticancer activity of α-, γ-, and δ-carboline natural products and their synthetic derivatives, as they provide new inroads for cancer therapy. Particularly, we highlight the new derivatives of α-, γ-, and δ-carboline with anticancer activity, and their anticancer mechanisms, as well as structure-activity relationship. Meanwhile, we propose strategies for the development of new α-, γ-, and δ-carboline derivatives for cancer therapy.
format Article
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institution OA Journals
issn 2772-4174
language English
publishDate 2024-12-01
publisher Elsevier
record_format Article
series European Journal of Medicinal Chemistry Reports
spelling doaj-art-2dd5d27238e44009b1187db24cf360172025-08-20T02:30:42ZengElsevierEuropean Journal of Medicinal Chemistry Reports2772-41742024-12-011210022110.1016/j.ejmcr.2024.100221Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARsJingliang Cui0Wanru Gao1Ziwei Liu2Shuang Cao3Sihui Long4Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, ChinaKey Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, ChinaKey Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, ChinaCorresponding author.; Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, ChinaCorresponding author.; Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, ChinaCarboline consists of a pyridine ring fused with an indole skeleton, and it serves as a potential drug scaffold. Depending on the relative position of the pyridine N to the indole N, carbolines can be categorized into α-, β-, γ-, and δ-subfamilies. They have diverse pharmacological activities, such as anticancer, antimalaria, antibacterial, antifungal, anti-Alzheimer's disease, etc. Among them, β-carbolines are the most widely studied and are also well reviewed. Herein, we review the anticancer activity of α-, γ-, and δ-carboline natural products and their synthetic derivatives, as they provide new inroads for cancer therapy. Particularly, we highlight the new derivatives of α-, γ-, and δ-carboline with anticancer activity, and their anticancer mechanisms, as well as structure-activity relationship. Meanwhile, we propose strategies for the development of new α-, γ-, and δ-carboline derivatives for cancer therapy.http://www.sciencedirect.com/science/article/pii/S2772417424000931α-, γ-, δ-carbolineDerivativesAnticancer activitySARMechanismStrategies
spellingShingle Jingliang Cui
Wanru Gao
Ziwei Liu
Shuang Cao
Sihui Long
Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs
European Journal of Medicinal Chemistry Reports
α-, γ-, δ-carboline
Derivatives
Anticancer activity
SAR
Mechanism
Strategies
title Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs
title_full Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs
title_fullStr Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs
title_full_unstemmed Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs
title_short Anticancer α-, γ-, and δ-carboline derivatives: structures, mechanisms of action, and SARs
title_sort anticancer α γ and δ carboline derivatives structures mechanisms of action and sars
topic α-, γ-, δ-carboline
Derivatives
Anticancer activity
SAR
Mechanism
Strategies
url http://www.sciencedirect.com/science/article/pii/S2772417424000931
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AT wanrugao anticanceraganddcarbolinederivativesstructuresmechanismsofactionandsars
AT ziweiliu anticanceraganddcarbolinederivativesstructuresmechanismsofactionandsars
AT shuangcao anticanceraganddcarbolinederivativesstructuresmechanismsofactionandsars
AT sihuilong anticanceraganddcarbolinederivativesstructuresmechanismsofactionandsars