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Thiazolo[4,5-]pyrimidine derivatives are considered potential therapeutic agents, particularly in the development of anticancer drugs. In this study, new 7-oxo-(), 7-chloro-() and also three 7-amino-() 5-trifluoromethyl-2-thioxo-thiazolo[4,5-]pyrimidine derivatives have been synthesized and evaluated for their potential anticancer activity. These derivatives were characterized by spectroscopic methods and elemental analysis, and the single-crystal X-ray diffraction was further performed to confirm a 3D structure for compounds and . The antiproliferative activity evaluation of twelve new compounds was carried out on a variety of cell lines including four human cancer (A375, C32, DU145, MCF-7/WT) and two normal cell lines (CHO-K1 and HaCaT). Four of them (, , and ) were selected by the National Cancer Institute and evaluated for their in vitro anticancer activity using the NCI-60 screening program. 7-Chloro-3-phenyl-5-(trifluoromethyl)[1,3]thiazolo[4,5-]pyrimidine-2(3)-thione () proved to be the most active among the newly synthesized compounds.
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http://dx.doi.org/10.3390/ph15010092 | 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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