Synthesis and Structure–Activity Relationships of Tetrahydro-β-carboline Derivatives as Anticancer and Cancer-chemopreventive Agents

Zhang, Mingming; Park, Eun-Jung; Kondratyuk, Tamara P.; Pezzuto, John M.; Sun, Dianqing

doi:10.21873/anticanres.12744

Cited by 14 publications

(8 citation statements)

References 19 publications

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“…According to the National Cancer Institute's preclinical cytotoxicity screening, 0.1 % of tested land samples and 1 % of tested marine samples had antitumor potential. [132] Zhang, et al [133] also conducted a study to find β-carboline derivatives with promise for cancer chemoprevention and treatment. [133] Scientists are intrigued by the natural product-like molecules created through the synthetic renewal of these natural products as semi-synthetic variants.…”

Section: Discussionmentioning

confidence: 99%

“…[132] Zhang, et al [133] also conducted a study to find β-carboline derivatives with promise for cancer chemoprevention and treatment. [133] Scientists are intrigued by the natural product-like molecules created through the synthetic renewal of these natural products as semi-synthetic variants. The important family of indole-based alkaloids known as β-carbolines has a wide range of anticancer properties that work through various mechanisms by interacting with various enzymes, targets, and receptors.…”

Section: Discussionmentioning

confidence: 99%

“…According to the National Cancer Institute's preclinical cytotoxicity screening, 0.1 % of tested land samples and 1 % of tested marine samples had antitumor potential [132] . Zhang, et al [133] . also conducted a study to find β‐carboline derivatives with promise for cancer chemoprevention and treatment [133] .…”

Section: Discussionmentioning

confidence: 99%

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Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Tshikhudo,

Mabhaudhi,

Koorbanally

et al. 2024

Chemistry & Biodiversity

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This comprehensive review is designed to evaluate the anticancer properties of β‐carbolines derived from medicinal plants, with the ultimate goal of assessing their suitability and potential in cancer treatment, management, and prevention. An exhaustive literature survey was conducted on a wide array of β‐carbolines including, but not limited to, harmaline, harmine, harmicine, harman, harmol, harmalol, pinoline, tetrahydroharmine, tryptoline, cordysinin C, cordysinin D, norharmane, and perlolyrine. Various analytical techniques were employed to identify and screen these compounds, followed by a detailed analysis of their anticancer mechanisms. Natural β‐carbolines such as harmaline and harmine have shown promising inhibitory effects on the growth of cancer cells, as evidenced by multiple in vitro and in vivo studies. Synthetically derived β‐carbolines also displayed noteworthy anticancer, neuroprotective, and cognitive‐enhancing effects. The current body of research emphasizes the potential of β‐carbolines as a unique source of bioactive compounds for cancer treatment. The diverse range of β‐carbolines derived from medicinal plants can offer valuable insights into the development of new therapeutic strategies for cancer management and prevention.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Tshikhudo,

Mabhaudhi,

Koorbanally

et al. 2024

Chemistry & Biodiversity

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Section: Direct Chemopreventive Agentsmentioning

confidence: 99%

“…β-Carboline molecules work as chemopreventive and chemotherapeutic agents. 49 β-Carboline alkaloid enriched extract from Rauwolfia vomitoria has been reported to have anti-prostate cancer activity. 50 Vitamin A, curcumin, isothiocyanate, green tea, luteolin, resveratrol, genistein, lycopene, bitter melon, withaferin A, and guggulsterone have been proposed for the chemoprevention of head and neck squamous cell carcinoma (HNSCC).…”

Section: Direct Chemopreventive Agentsmentioning

confidence: 99%

Natural Products as Cancer Chemo Preventive Agents: Where We Stand

Boretti¹

2022

Natural Product Communications

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This work briefly reviews cancer chemoprevention. This is a very challenging field, as products with a high level of toxicity such as chemotherapeutic agents may be proposed and accepted only under life-threatening conditions. Cancer chemoprevention is otherwise limited to completely safe substances, preferably having neither toxic nor side effects, administered in relatively low amounts. Phases of clinical trials, therapeutic end-points, and biomarkers of chemoprevention are difficult to be defined. The clinical trials needed to prove the efficacy of chemopreventive agents must be very long and extremely widespread to achieve significance, with many variables difficult to control, and therefore subjected to many confounding factors. This makes them almost impossible. It is, therefore, no surprise, if the progress of chemoprevention has been so far very limited. There are only a few examples of direct use of chemopreventive agents, under investigation, but with anything but established protocols, in addition to indirect uses such as general supplementation with antioxidant, anti-inflammatory, and immune-supportive agents. Cancer chemoprevention remains a potentially very rewarding approach, certainly worth further study, but extremely difficult to pursue, in need of different methodological approaches to producing valuable chemopreventive compounds of clear dosages and benefits.

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Synthesis, structure–activity relationship, and biological evaluation of quinolines for development of anticancer agents

Wang

et al. 2023

Archiv der Pharmazie

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Tetrahydro‐β‐carbolines (THβCs) are a kind of natural alkaloids with multiple pharmaceutical activities. Herein, a focused compound library derived from THβCs was synthesized and their anticancer activities were studied in several cancer cell lines. Among them, three compounds showed considerable anticancer activities with low micromolar to submicromolar IC50 values. The abilities to induce apoptosis and alter mitochondrial membrane potential levels, which are comparable to those of the commercial anticancer drug adriamycin, were confirmed by one representative compound (21) on the B16/F10 cell line. Our preliminary structure–activity relationship studies indicated that alkylamines with suitable lengths are very important for potency improvement.

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Synthesis and Structure–Activity Relationships of Tetrahydro-β-carboline Derivatives as Anticancer and Cancer-chemopreventive Agents

Cited by 14 publications

References 19 publications

Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Natural Products as Cancer Chemo Preventive Agents: Where We Stand

Synthesis, structure–activity relationship, and biological evaluation of quinolines for development of anticancer agents

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