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Anti-Cancer Drugs: Natural Products, Synthetic Compounds and Potential Pharmacological Effects and Applications

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (20 June 2025) | Viewed by 3463

Special Issue Editors


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Guest Editor
Key Laboratory of Protein Chemistry and Developmental Biology of State Ministry of Education, College of Life Sciences, Hunan Normal University, Changsha 410081, China
Interests: anti-cancer; mechanism; animal model; pharmacological action; inhibitor; drug target; cancer stem cell

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Guest Editor
Key Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha 410013, China
Interests: natural product; bioactive constituents; synthetic compound; small-molecule inhibitor; pharmacological action; drug development; mechanism

Special Issue Information

Dear Colleagues,

Anti-cancer drug research lies in the fact that it not only provides us with effective treatment options to combat cancer but also significantly improves patients' survival rates and quality of life. As the incidence of cancer continues to rise, the development of new anti-tumor drugs has become particularly urgent. These studies involve not only the discovery and development of new drugs but also the improvement of existing medications to overcome resistance and side effects. Furthermore, anti-cancer drug research drives advancements in the biomedical field and promotes the development of personalized medicine, allowing treatment plans to be adjusted based on the specific conditions and genetic characteristics of patients, thereby achieving more precise therapeutic effects. Through continuous research and innovation, we hope to find more effective treatment methods.

Natural small-molecule drugs typically originate from plants, microorganisms, or animals, featuring complex chemical structures and diverse biological activities. They can exert anti-tumor effects through various mechanisms, such as by inducing apoptosis, inhibiting tumor cell proliferation, and preventing metastasis. Natural small-molecule drugs hold an important position in the field of anti-tumor drug research. Synthetic small-molecule drugs are prepared through chemical synthesis methods, offering better controllability and consistency. The design of synthetic drugs can target specific sites, optimizing their efficacy and safety, thereby enhancing therapeutic effects. Although synthetic small-molecule drugs offer high flexibility and predictability in drug development, they may also face issues such as drug resistance and side effects.

In this Special Issue of the International Journal of Molecular Sciences, we will discuss natural and synthetic compounds with anti-cancer properties, including their discovery, synthesis, structural modification, pharmacological actions and mechanisms, and their potential clinical values.

Dr. Kaiqun Ren
Dr. Hui Zou
Guest Editors

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Keywords

  • cancer
  • natural product
  • synthetic compounds
  • mechanism
  • structural modification
  • pharmacological action

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Published Papers (2 papers)

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Review

22 pages, 1665 KiB  
Review
Molecular Mechanisms of Vitexin: An Update on Its Anti-Cancer Functions
by Liyun Lu, Yinhua Deng, Junnan Li, Xing Feng and Hui Zou
Int. J. Mol. Sci. 2025, 26(12), 5853; https://doi.org/10.3390/ijms26125853 - 18 Jun 2025
Viewed by 774
Abstract
Cancer remains a leading global health challenge, necessitating the exploration of novel therapeutic strategies. Vitexin (apigenin-8-C-β-D-glucopyranoside), a natural flavonoid glycoside with a molecular weight of 432.38 g/mol, is derived from plants such as mung bean, beetroot, and hawthorn. This compound features a distinctive [...] Read more.
Cancer remains a leading global health challenge, necessitating the exploration of novel therapeutic strategies. Vitexin (apigenin-8-C-β-D-glucopyranoside), a natural flavonoid glycoside with a molecular weight of 432.38 g/mol, is derived from plants such as mung bean, beetroot, and hawthorn. This compound features a distinctive C-glycosidic bond at the 8-position of its apigenin backbone, contributing to its enhanced metabolic stability compared to O-glycosidic flavonoids. Preclinical studies demonstrate that vitexin modulates critical cellular processes such as cell cycle progression, apoptosis, autophagy, metastasis, angiogenesis, epigenetic modifications, and tumor glycolysis inhibition. It exerts its effects by targeting key signaling pathways, including phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin (PI3K/Akt/mTOR), nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), and signal transducer and activator of transcription 3 (STAT3), and shows potential for combination therapies to enhance efficacy and overcome resistance. Advances in nanotechnology further enhance its bioavailability and delivery potential. This review comprehensively examines the current evidence on vitexin’s anticancer mechanisms, highlighting its multi-target therapeutic potential and future research directions. Full article
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17 pages, 844 KiB  
Review
Small Molecule B-RAF Inhibitors as Anti-Cancer Therapeutics: Advances in Discovery, Development, and Mechanistic Insights
by Yamile Abuchard Anaya, Ricardo Pequeno Bracho, Subhash C. Chauhan, Manish K. Tripathi and Debasish Bandyopadhyay
Int. J. Mol. Sci. 2025, 26(6), 2676; https://doi.org/10.3390/ijms26062676 - 16 Mar 2025
Cited by 1 | Viewed by 2258
Abstract
B-RAF is a serine/threonine kinase that plays a crucial role in the MAPK signaling pathway, regulating cell proliferation and survival. Mutations in B-RAF, particularly V600E, are associated with several malignancies, including melanoma, colorectal cancer, and non-small cell lung cancer, making it a key [...] Read more.
B-RAF is a serine/threonine kinase that plays a crucial role in the MAPK signaling pathway, regulating cell proliferation and survival. Mutations in B-RAF, particularly V600E, are associated with several malignancies, including melanoma, colorectal cancer, and non-small cell lung cancer, making it a key therapeutic target. The development of B-RAF inhibitors, such as Vemurafenib, Dabrafenib, and second-generation inhibitors like Encorafenib, has led to significant advancements in targeted cancer therapy. However, acquired resistance, driven by MAPK pathway reactivation, RAF dimerization, and alternative signaling pathways, remains a major challenge. This review explores the molecular mechanisms of B-RAF inhibitors, their therapeutic efficacy, and resistance mechanisms, emphasizing the importance of combination strategies to enhance treatment outcomes. The current standard of care involves B-RAF and MEK inhibitors, with additional therapies such as EGFR inhibitors and immune checkpoint blockades showing potential in overcoming resistance. Emerging pan-RAF and brain-penetrant inhibitors offer new opportunities for treating refractory cancers, while precision medicine approaches, including genomic profiling and liquid biopsies, are shaping the future of B-RAF-targeted therapy. Full article
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