ArticleACS medicinal chemistry letters2013
Antitumor potential of conjugable valinomycins bearing hydroxyl sites: in vitro studies.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
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- Identification ofMicrobiology spectrum · 2023Article
- Direct Synthesis of 3-Aryl Substituted Isocoumarins and Phthalides through Palladium Acetate Catalyzed C(spChemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Applications and Restrictions of Integrated Genomic and Metabolomic Screening: An Accelerator for Drug Discovery from Actinomycetes?Molecules (Basel, Switzerland) · 2021Review
- The Nonribosomal Peptide Valinomycin: From Discovery to Bioactivity and Biosynthesis.Microorganisms · 2021Review
- Therapeutic Potential of Exploiting Autophagy Cascade Against Coronavirus Infection.Frontiers in microbiology · 2021Review
- Valinomycin as a potential antiviral agent against coronaviruses: A review.Biomedical journal · 2020Review
- Potassium-Ion-Selective Fluorescent Sensors To Detect Cereulide, the Emetic Toxin ofChemistryOpen · 2017Article
Corrections and comments
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Authors and funding
9 authors.
Funding
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Abstract
Following our pioneering studies on the direct and efficient introduction of derivatizable hydroxyl handles into the valinomycin (VLM, 1) structure, a K(+)-ionophore with potent antitumor activity, the ensuing conjugable analogues (HyVLMs 2, 3, and 4) have herein been compared to the parent macrocycle for their potential antiproliferative effects on a panel of cancer cell lines, namely, human MCF-7, A2780, and HepG2, as well as rat C6 cells. On the basis of IC50 values, we find that hydroxyl analogues 3 and 4 are only moderately less active than 1, while analogue 2 experiences a heavily diminished activity. Cytofluorimetric analyses of MCF-7 cells treated with HyVLMs suggest that the latter depolarize mitochondria, thus retaining the typical VLM behavior. It is likely that C6 cells, for which the exceptionally potent cytotoxicity of VLM has never reported previously, follow the same fate, as evidenced by alteration of mitochondrial morphology upon incubation with each ionophore.
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