Undoubtedly, efficient cancer treatment has been a significant challenge for the scientific community over the last decades. Despite tremendous progress made towards this direction, there are still efforts needed to discover new anticancer drugs. In this work, a series of N-substituted pyrrolebased scaffolds have been synthesized and evaluated for antiproliferative activity against a panel of cancer cell lines (L1210, CEM and HeLa). Furthermore, in order to discover new scaffolds as antiviral agents, all the examined compounds were evaluated for activity against different types of DNA and RNA viruses. The key feature of the above structures is the existence of an aromatic ring with at least one hydrogen-bonding donor and acceptor group. Results have shown noteworthy cytostatic activity for three of the synthesized compounds (1, 3 and 9). Especially, compound 1, containing a tropolone ring, proved to be the most promising scaffold (IC50:10-14 µM) for the development of novel potential anticancer agents. In addition, compound 1 has shown modest anti-HSV-1, -HSV2 activity in HEL cell cultures (EC50: 27-40 µM).
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http://dx.doi.org/10.2174/1573406411666150313161225 | DOI Listing |
J Cell Mol Med
January 2025
Department of Molecular Biology and Genetics, Faculty of Arts and Sciences, Yildiz Technical University, Istanbul, Turkiye.
siRNA-loaded nanoparticles open new perspectives for cancer treatment. MAPK6 is upregulated in breast cancer and is involved in cell growth, differentiation and cell cycle regulation. Herein, we aimed to investigate the anticancer effects of MAPK6 knockdown by using MAPK6 siRNA-loaded PLGA nanoparticles (siMAPK6-PLGA-NPs) in MCF-7 breast cancer cells.
View Article and Find Full Text PDFDose Response
January 2025
Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Saud University, Riyadh, Saudi Arabia.
Cytokinins are plant hormones that regulate cell growth and differentiation. In particular, zeatin (ZTN) delays cellular senescence of human fibroblasts and keratinocytes and exhibits anticancer activity. Chemotherapy-induced anemia is a major side effect of anticancer therapy secondary to premature senescence of red blood cells (RBCs).
View Article and Find Full Text PDFChem Sci
January 2025
Université Paris-Saclay, CNRS, Institut Galien Paris-Saclay 91400 Orsay France +33-180006081.
The synthesis of degradable polymer prodrug nanoparticles is still a challenge to be met, which would make it possible to remedy both the shortcomings of traditional formulation of preformed polymers (, low nanoparticle concentrations) and those of the physical encapsulation of drugs (, burst release and poor drug loadings). Herein, through the combination of radical ring-opening polymerization (rROP) and polymerization-induced self-assembly (PISA) under appropriate experimental conditions, we report the successful preparation of high-solid content, degradable polymer prodrug nanoparticles, exhibiting multiple drug moieties covalently linked to a degradable vinyl copolymer backbone. Such a rROPISA process relied on the chain extension of a biocompatible poly(ethylene glycol)-based solvophilic block with a mixture of lauryl methacrylate (LMA), cyclic ketene acetal (CKA) and drug-bearing methacrylic esters by reversible addition fragmentation chain transfer (RAFT) copolymerization at 20 wt% solid content.
View Article and Find Full Text PDFChem Biodivers
January 2025
Shanghai Pudong New Area Public Interest Hospital: Shanghai Pudong New Area Gongli Hospital, Department of Pharmacy, 219 Miaopu Road, Shanghai, CHINA.
Natural products (NPs) play a crucial role in drug discovery, with over 30% of recent FDA-approved drugs derived from them. Plants from the genus Goniothalamus, belonging to the Annonaceae family, have garnered significant interest as potential sources of active lead compounds. Over the past five decades, researchers have isolated 357 compounds from Goniothalamus species (GCs), which exhibit a wide range of pharmacological properties, including cytotoxicity, antibacterial, antifungal, antiplasmodial, antioxidant, and other activities.
View Article and Find Full Text PDFMed Oncol
January 2025
Department of Medical Pharmacology, Medical Faculty, Atatürk University, Erzurum, Turkey.
Limited advancements in managing malignant brain tumors have resulted in poor prognoses for glioblastoma (GBM) patients. Standard treatment involves surgery, radiotherapy, and chemotherapy, which lack specificity and damage healthy brain tissue. Boron-containing compounds, such as boric acid (BA), exhibit diverse biological effects, including anticancer properties.
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