Four new withanolides (2-5), together with 4β,7β,20-trihydroxy-1-oxowitha-2,5,24-trienolide (1), were isolated from the aerial parts of Eriolarynx iochromoides. The antiproliferative activity of all compounds purified from E. iochromoides together with four withaphysalins and four physangulidines isolated previously from three Deprea species were evaluated against human solid tumor cell lines. Four withanolides showed antiproliferative activity comparable in potency to cisplatin. Selectivity toward cancer cells and interaction with P-glycoprotein of the active withanolides were evaluated.
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http://dx.doi.org/10.1021/acs.jnatprod.9b00117 | DOI Listing |
Chem Biol Drug Des
January 2025
Faculty of Pharmacy in Hradec Králové, Charles University, Hradec Králové, Czech Republic.
Infectious diseases, including bacterial, fungal, and viral, have once again gained urgency in the drug development pipeline after the recent COVID-19 pandemic. Tuberculosis (TB) is an old infectious disease for which eradication has not yet been successful. Novel agents are required to have potential activity against both drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis (Mtb), the causative agent of TB.
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January 2025
Department of Life Science and Agriculture, Zhoukou Normal University Zhoukou Henan 466001 China
This study reports a green, multi-component synthesis of 2-aminoimidazole-linked quinoxaline Schiff bases using a novel superparamagnetic acid catalyst. The catalyst consists of sulfo-anthranilic acid (SAA) immobilized on MnCoFeO@alginate magnetic nanorods (MNRs), achieving high SAA loading (1.8 mmol g) and product yields (91-97%).
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January 2025
Department of Pharmaceutical Sciences, Maharshi Dayanand University Rohtak 124001 India
Cancer is a major global concern. Despite considerable advancements in cancer therapy and control, there are still large gaps and requirements for development. In recent years, various naturally occurring anticancer drugs have been derived from natural resources, such as alkaloids, glycosides, terpenes, terpenoids, flavones, and polyphenols.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Biochemistry, Panjab University, Chandigarh 160014, India.
Over the years, numerous ligand-based organotin(IV) Schiff base compounds have shown remarkable cytotoxicity and anticancer activities, but their clinical use is restricted by systemic toxicity, prompting the search for targeted therapies. Targeted delivery can be enhanced by exploiting the inherent characteristics of cancer cells such as glutamine addiction, which is essential to support cellular biosynthesis and cell growth to sustain aberrant proliferation. Our previous study revealed glutamine-conjugated organotin(IV) compounds have strong DNA/protein affinities, favorable in silico ADME profiles, and significant antiproliferative activity.
View Article and Find Full Text PDFEur J Med Chem
January 2025
School of Pharmaceutical Sciences, Guizhou University, Guiyang, 550025, China. Electronic address:
Temozolomide, a widely used alkylating agent for glioblastoma treatment, faces significant challenges due to the development of resistance, which severely impacts patient survival. This underscores the urgent need for novel strategies to overcome this barrier. Focal adhesion kinase (FAK), an intracellular non-receptor tyrosine kinase, is highly expressed in glioblastoma cells and has been identified as a promising therapeutic target for anti-glioblastoma drug development.
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