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The triazole functional group plays a pivotal role in the composition of biomolecules with potent anticancer activities, including numerous clinically approved drugs. The strategic utilization of the triazole fragment in the rational modification of lead compounds has demonstrated its ability to improve anticancer activities, enhance selectivity, optimize pharmacokinetic properties, and overcome resistance. There has been significant interest in triazole-containing hybrids in recent years due to their remarkable anticancer potential. However, previous reviews on triazoles in cancer treatment have failed to provide tailored design strategies specific to these compounds. Herein, we present an overview of design strategies encompassing a structure-modification approach for incorporating triazoles into hybrid molecules. This review offers valuable references and briefly introduces the synthesis of triazole derivatives, thereby paving the way for further research and advancements in the field of effective and targeted anticancer therapies.
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http://dx.doi.org/10.1016/j.ejmech.2024.116578 | DOI Listing |
Chem Res Toxicol
September 2025
University of Texas Medical Branch, Galveston, Texas 77555, United States.
Glioblastoma (GBM) is a lethal brain tumor with limited therapeutic options. Temozolomide (TMZ), a standard-of-care chemotherapeutic agent, exerts its cytotoxicity by alkylating DNA, which triggers a DNA damage response and depletes ATP and NAD. However, TMZ also releases the byproduct 4-amino-5-imidazole carboxamide (AIC), which is believed to be a benign metabolite.
View Article and Find Full Text PDFEur J Med Chem
August 2025
School of Chemistry and Chemical Engineering, Anhui University of Technology, Ma'anshan, 243032, Anhui, PR China. Electronic address:
Cancer remains a leading global cause of mortality, with treatment efficacy often compromised by drug resistance, highlighting the urgent need for novel targeted therapies. The enzyme fructose-2,6-bisphosphatase 4 (PFKFB4) governs glycolytic flux by modulating fructose-2,6-bisphosphate (F2,6BP) levels. PFKFB4 overexpression has been observed in various cancers and correlates with tumor growth, aggressiveness, and poor prognosis.
View Article and Find Full Text PDFRetina
September 2025
School of Mathematical and Computational Sciences, University of Prince Edward Island, Charlottetown, Canada.
Purpose: Systemically administered anti-cancer VEGF inhibiting therapies can cause severe kidney injury. Intravitreal aflibercept has a greater impact on renal VEGF levels than ranibizumab. We compared the risk of kidney injury among patients receiving intravitreal aflibercept vs.
View Article and Find Full Text PDFMed Oncol
September 2025
Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt.
Gynecological cancer, encompassing cancers such as endometrial and cervical cancer, is a growing concern worldwide, with a rising incidence and significant impact on women's health. Pterostilbene (PT), a natural compound, has shown promising therapeutic potential in gynecological cancer treatment. This review aims to summarize the current state of knowledge on PT's effects in gynecological cancer, focusing on its molecular mechanisms, preclinical studies, and clinical trials.
View Article and Find Full Text PDFArch Pharm Res
September 2025
Department of Biosciences, JIS University, 81, Nilgunj Road, Agarpara, Kolkata, West Bengal, 700109, India.
Bacoside A (BCA), a triterpenoid saponin isolated from Bacopa monnieri, exhibits diverse pharmacological properties, including neuroprotective, hepatoprotective, anti-stress, anti-inflammatory, and anti-ulcer effects. In the present study, BCA demonstrates pronounced anticancer activity against K562 chronic myelogenous leukemia (CML) cells by modulating autophagy-apoptosis dynamics. BCA induces dose- and time-dependent cytotoxicity in K562 cells while sparing normal human peripheral blood mononuclear cells (hPBMCs) and Vero cells, indicating therapeutic selectivity.
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