A series of new flavone/isoxazole fused heterocycles 5a-f and flavone/1,2,3-triazole/benzimidazole hybrid heterocycles compounds 7a-t were synthesized via an intramolecular cyclization and Cu(I)-catalyzed click 1,3-dipolar cycloaddition. The products were evaluated for their antiproliferative activity against human breast cancer cell line (MCF-7) using sulforhodamine B assay (SRB) and antimycobacterial activity using turbidometric assay. The majority of the tested compounds exhibited antiproliferative activity and antimycobacterial activity. Compounds 7l, 7q and 7r showed moderate antiproliferative activity with IC50 values 17.9, 14.2, 19.1 [Formula: see text], respectively, and compound 5a showed moderate antimycobacterial activity with 41.7% of inhibition at 30 [Formula: see text] concentration.
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http://dx.doi.org/10.1007/s11030-018-9833-4 | DOI Listing |
Reprod Sci
December 2024
Department of Gynecology and Obstetrics, Division of Reproductive Sciences & Women's Health Re-search, Johns Hopkins Medicine, Baltimore, MD, 21205, USA.
Pomegranate (Punica granatum) is a widely cultivated fruit historically recognized for its health benefits and is regarded as a nutritional powerhouse. Pomegranate has a unique composition of bioactive compounds including hydrolysable tannins, anthocyanins, and other polyphenolic components. Of those, punicalagin and its subsequent metabolites are the most extensively studied, demonstrating antioxidant, anti-inflammatory, anti-cancer, and anti-nociceptive activity.
View Article and Find Full Text PDFSci Rep
December 2024
Department of Life Sciences, College of Life Sciences, National Chung Hsing University, Kuo Kuang Rd., Taichung, 402, Taiwan.
Hepatocellular carcinoma (HCC) constitutes 90% of liver cancer cases and ranks as the third leading cause of cancer-related mortality, necessitating urgent development of alternative therapies. Lactoferrin (LF), a natural iron-binding glycoprotein with reported anticancer effects, is investigated for its potential in liver cancer treatment, an area with limited existing studies. This study focuses on evaluating LF's anti-liver cancer effects on HCC cells and assessing the preventive efficacy of oral LF administration in a murine model.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
BioLab, Instituto Universitario de Bio-Orgánica "Antonio González", University of La Laguna, La Laguna, Spain.
Glycosylation patterns represent an important signature of cancer cells that can be decoded by glycan-binding proteins, i.e., lectins.
View Article and Find Full Text PDFJ Med Chem
December 2024
Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Rearranged during transfection (RET) kinase is a validated therapeutic target for various cancers characterized by RET alterations. Although two selective RET inhibitors, selpercatinib and pralsetinib, have been approved by the FDA, acquired resistance through solvent-front mutations has been identified rapidly. Developing proteolysis targeting chimera (PROTAC) targeting RET mutations offers a promising strategy to combat drug resistance.
View Article and Find Full Text PDFJ Org Chem
December 2024
Department of Pharmacy, The First Affiliated Hospital, Jinan University, Guangzhou 510630, China.
Nine new structurally diverse filicinic acid-based meroterpenoids (-) with four kinds of carbon skeletons were isolated from the rhizomes of . Their structures, including the absolute configurations, were elucidated by comprehensive analysis of spectroscopic data, quantum chemical calculations, and single-crystal X-ray diffraction. Structurally, compounds - feature an unprecedented 6/6/5/6/6/6 hexacyclic system with a rare oxaspiro[4.
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