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Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 25, Issue 5, 2025

Volume 25, Issue 5

Volume 25, Issue 5, 2025

    • Molecular Targets of Plant-based Alkaloids and Polyphenolics in Liver and Breast Cancer- An Insight into Anticancer Drug Development

      https://doi.org/10.2174/0118715206302216240628072554

      Liver and Breast cancer are ranked as the most prevailing cancers that cause high cancer-related mortality. As cancer is a life-threatening disease that affects the human population globally, there is a need to develop novel therapies. Among the available treatment options include radiotherapy, chemotherapy, surgery, and immunotherapy. The most superlative modern method is the use of plant-derived anticancer drugs that target the cancerous cells and inhibit their proliferation. Plant-derived compounds are generally considered safer than synthetic drugs/traditional therapies and could serve as potential novel targets to treat liver and breast cancer to revolutionize cancer treatment. Alkaloids and Polyphenols have been shown to act as anticancer agents through molecular approaches. They disrupt various cellular mechanisms, inhibit the production of cyclins and CDKs to arrest the cell cycle, and activate the DNA repairing mechanism by upregulating p53, p21, and p38 expression. In severe cases, when no repair is possible, they induce apoptosis in liver and breast cancer cells by activating caspase-3, 8, and 9 and increasing the Bax/Bcl-2 ratio. They also deactivate several signaling pathways, such as PI3K/AKT/mTOR, STAT3, NF-κB, Shh, MAPK/ERK, and Wnt/β-catenin pathways, to control cancer cell progression and metastasis. The highlights of this review are the regulation of specific protein expressions that are crucial in cancer, such as in HER2 over-expressing breast cancer cells; alkaloids and polyphenols have been reported to reduce HER2 as well as MMP expression. This study reviewed more than 40 of the plant-based alkaloids and polyphenols with specific molecular targets against liver and breast cancer. Among them, Oxymatrine, Hirsutine, Piperine, Solamargine, and Brucine are currently under clinical trials by qualifying as potent anticancer agents due to lesser side effects. As a lot of research is there on anticancer compounds, there is a desideratum to compile data to move towards clinical trials phase 4 and control the prevalence of liver and breast cancer.

    • Curcumin and its Analogues in Oral Squamous Cell Carcinoma: State-of-the-art and Therapeutic Potential

      https://doi.org/10.2174/0118715206297840240510063330

      Oral Squamous Cell Carcinoma (OSCC) is the most common cancer arising from squamous epithelium in the oral cavity and is characterized by high aggressiveness and metastatic potential, which together with a late diagnosis results in a 5-year survival rate of only 50% of patients. The therapeutic options for OSCC management are limited and largely influenced by the cancer stage. While radical surgery can be curative in early stage of disease, most cases require adjuvant therapies, including chemotherapy and radiotherapy which, however, often achieve poor curative rates and are associated with important negative effects. Therefore, there is an urgent need to discover new alternative treatment strategies to improve patients’ outcomes. Several medicinal herbs are being studied for their preventive or therapeutic effect in several diseases, including cancer. In particular, the Indian spice curcumin, largely used in oriental countries, has been studied as a chemopreventive or adjuvant agent for different malignancies. Indeed, curcumin is characterized by important biological properties, including antioxidant, anti-inflammatory, and anticancer effects, which could also be exploited in OSCC. However, due to its limited bioavailability and poor aqueous solubility, this review is focused on studies designing new synthetic analogues and developing novel types of curcumin delivery systems to improve its pharmacokinetic and biological properties. Thus, this review analyses the potential therapeutic role of curcumin in OSCC by providing an overview of current and studies demonstrating the beneficial effects of curcumin and its analogues in OSCC.

    • Urea and Thiourea Derivatives of Salinomycin as Agents Targeting Malignant Colon Cancer Cells

      https://doi.org/10.2174/0118715206322603241002064435
      Background

      Since it was discovered that a natural polyether ionophore called salinomycin () selectively inhibits human cancer cells, the scientific world has been paying special attention to this compound. It has been studied for nearly 15 years.

      Objective

      Thus, a very interesting research direction is the chemical modification of structure, which could give more biologically active agents.

      Methods

      We evaluated the anticancer activity of (thio)urea analogues class of C20--aminosalinomycin (compound ). The studies covered the generation of reactive oxygen species (ROS), proapoptotic activity, cytotoxic activity, and lipid peroxidation .

      Results

      Thioureas showed antiproliferative activity against selected human colon cancer cell lines greater than that of chemically unmodified , with a 2~10-fold higher potency towards a metastatic variant of colon cancer cells (SW620). Mechanistically, derivatives showed proapoptotic activity in primary colon cancer cells and induced the production of reactive oxygen species (ROS) in these cells. In SW620 cells, derivatives increased lipid peroxidation with a weak effect on apoptosis and low ROS formation with cytotoxic effects followed by cytostatic ones, suggesting different modes of action of the compounds against primary and metastatic colon cancer cells.

      Conclusion

      The results of this study suggested that urea and thiourea derivatives of provide promising leads for the rational development of new anticancer active agents.

    • Current Insights into Therapeutic Potential of Terpenoids as Anticancer Agents

      https://doi.org/10.2174/0118715206342920241008062115
      Background

      Cancer is regarded as one of the main causes of death globally. Future predictions indicate that the death rate from cancer will keep rising, which may reach 11.4 million in 2030. Carcinogenesis refers to the phenomenon of transforming a normal cell into a cancer cell. Cancer is characterized by unregulated and uncontrolled cell division due to alterations at the molecular and genetic levels. Gene mutations can speed up the rate of cell division, which leads to cancer. Metastasis entails the dissemination of cancer cells from the primary site to distant regions of the body the circulatory or lymphatic systems.

      Objective

      This review is mainly focusing on the anticancer properties of terpenoids. In the case of human beings, several types of cancers can be treated clinically based on the form and phase of the cancer. So, there are different types of treatment regimens available for the management of cancer, such as immunotherapy, hormonal therapy, radiation therapy, and chemotherapy.

      Methods

      Several problems are associated with cancer therapy, including chemoresistance, severe toxicity, relapse, and metastasis. To minimize these complications, natural products like terpenoids seem to be beneficial for the effective management of cancer.

      Results

      Experimental results revealed that the anticancer potential of terpenoids is due to activation of apoptosis and stimulation of cell cycle arrest. Some of the terpenoids exhibit anticancer effects by inhibiting angiogenesis and metastasis the regulation of several signaling pathways intracellularly. Certain terpenoids have been shown to work in concert with anticancer medications (doxorubicin, cisplatin, paclitaxel, and 5-fluorouracil) to provide synergistic effects. These terpenoids have also been shown to be effective against cancer cells that are resistant to several drug therapies.

      Conclusion

      The current study will focus on signaling pathways and mode of action of several types of terpenoids as anticancer agents. Further, it will provide insights into the ongoing clinical trials and prospective pathways for the advancement of terpenoids as possible anti-cancer agents.

    • A Novel Effective Models for Identifying BRCA Patients and Optimizing Clinical Treatments

      https://doi.org/10.2174/0118715206336019241119070155
      Objective

      This study aimed to develop an effective model that identifies high-risk breast cancer (BRCA) patients and optimizes clinical treatments.

      Methods

      This study includes five public datasets, TCGA-BRCA as the training dataset and other cohorts as the validation datasets. Machine learning algorithms for finding key tumor-associated immune gene pairs (TAIGPs). These TAIGPs were used to construct tumor-associated immune gene pair index (TAIGPI) by multivariate analysis and further validated on the validation datasets. In addition, the differences in clinical prognosis, biological characteristics, and treatment benefits between high and low TAIGPI groups were further analyzed.

      Results

      The TAIGPI was established by 36 TAIGPs. Better clinical outcomes in the low TAIGPI patients, with consistent results, were also obtained in the validation datasets. The study showed that patients in the low TAIGPI group had a high infiltration of immune cells and low proliferative activity of tumor cells. In contrast, patients in the high TAIGPI group exhibited low infiltration of immune cells and high proliferative activity of tumor cells. In addition, patients in the low TAIGPI group are more likely to benefit from chemotherapy, adjuvant chemotherapy, or immunotherapy.

      Conclusions

      The TAIGPI can be an effective predictive strategy for the clinical prognosis of breast cancer patients, providing new insights into personalized treatment options for breast cancer patients.

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