ArticleScientific reports2016
Synthesis and mechanisms of action of novel harmine derivatives as potential antitumor agents.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed, 65 citations in OpenAlex.
- Harmaline and the gut-brain-immune axis: a novel therapeutic avenue in neuroinflammation and ulcerative colitis.Inflammopharmacology · 2026Review
- Network pharmacology analysis and experimental validation of the gastric cancer-related targets of harmine.Scientific reports · 2026Article
- Efficacy and mechanism of action of harmine derivative H-2-104 against Echinococcus granulosus infection in mice.BMC veterinary research · 2025Article
- Anti-tumor potential of Harmine and its derivatives: recent trends and advancements.Discover oncology · 2025Review
- Hesperetin Inhibits Bladder Cancer Cell Proliferation and Promotes Apoptosis and Cycle Arrest by PI3K/AKT/FoxOCurrent medicinal chemistry · 2025Article
- Cytotoxicity of alkaloids isolated from Peganum harmala seeds on HCT116 human colon cancer cells.Molecular biology reports · 2024Article
- Evaluation of the Therapeutic Effects of Harmine on Anaplastic Thyroid Cancer Cells.International journal of molecular sciences · 2024Article
- Research progress on the antitumor effects of harmine.Frontiers in oncology · 2024Review
- Phloretin induces G2/M arrest and apoptosis by suppressing the β-catenin signaling pathway in colorectal carcinoma cells.Apoptosis : an international journal on programmed cell death · 2023Article
- Discovery of indole analogues fromFrontiers in pharmacology · 2023Article
- Article
- In vitro and in vivo Efficacies of Novel Harmine Derivatives in the Treatment of Cystic Echinococcosis.Drug design, development and therapy · 2023Article
- Anthranilamides with quinoline and β-carboline scaffolds: design, synthesis, and biological activity.Molecular diversity · 2022Article
- Naturally derived indole alkaloids targeting regulated cell death (RCD) for cancer therapy: from molecular mechanisms to potential therapeutic targets.Journal of hematology & oncology · 2022Review
- Role of Plant-Derived Active Constituents in Cancer Treatment and Their Mechanisms of Action.Cells · 2022Review
- Components ofMolecules (Basel, Switzerland) · 2022Article
- Harmine is an effective therapeutic small molecule for the treatment of cardiac hypertrophy.Acta pharmacologica Sinica · 2022Article
- Synthesis and Biological Evaluation of Harmirins, Novel Harmine-Coumarin Hybrids as Potential Anticancer Agents.Molecules (Basel, Switzerland) · 2021Article
- Article
- A 3D culture platform enables development of zinc-binding prodrugs for targeted proliferation of β cells.Science advances · 2020Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of novel harmine derivatives bearing a benzylindine substituent in position-1 of β-carboline ring were synthesized and evaluated as antitumor agents. The N2-benzylated β-carboline derivatives 3a-g represented the most interesting anticancer activities and compound 3c was found to be the most active agent to diverse cancer cell lines such as gastric carcinoma, melanoma and colorectal cancer. Notably, compound 3c showed low toxicity to normal cells. The treatment significantly induced cell apoptosis. Mechanistically, PI3K/AKT signaling pathway mediated compound 3c-induced apoptosis. Compound 3c inhibited phosphorylation of AKT and promoted the production of reactive oxygen species (ROS). The ROS scavenger, LNAC and GSH, could disturb the effect of compound 3c induced apoptosis and PI3K activity inhibitor LY294002 synergistically enhanced compound 3c efficacy. Moreover, the results from nude mice xenograft model showed that compound 3c treatment effectively inhibited tumor growth and decreased tumor weight. Collectively, our results demonstrated that compound 3c exerts apoptotic effect in cancer cells via suppression of phosphorylated AKT and evocation of ROS generation, which suggested that compound 3c might be served as a promising therapeutic agent for cancer treatment.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.