ArticleChemistry (Weinheim an der Bergstrasse, Germany)2014
Design of enzymatically cleavable prodrugs of a potent platinum-containing anticancer agent.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Fabrication strategies for chiral self-assembly surface.Mikrochimica acta · 2024Review
- Platinum-Acridine Agents with High Activity in Cancers Expressing the Solute Carrier MATE1 (ACS medicinal chemistry letters · 2023Article
- Stimuli-responsive platinum and ruthenium complexes for lung cancer therapy.Frontiers in pharmacology · 2022Review
- Evaluation of a Platinum-Acridine Anticancer Agent and Its Liposomal Formulation in an in vivo Model of Lung Adenocarcinoma.ChemMedChem · 2021Article
- Discovery of a Chiral DNA-Targeted Platinum-Acridine Agent with Potent Enantioselective Anticancer Activity.Angewandte Chemie (International ed. in English) · 2020Article
- A membrane transporter determines the spectrum of activity of a potent platinum-acridine hybrid anticancer agent.Scientific reports · 2020Article
- Cysteine-Directed Bioconjugation of a Platinum(II)-Acridine Anticancer Agent.Inorganic chemistry · 2019Article
- Large-Pore Functionalized Mesoporous Silica Nanoparticles as Drug Delivery Vector for a Highly Cytotoxic Hybrid Platinum-Acridine Anticancer Agent.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Linker design for the modular assembly of multifunctional and targeted platinum(ii)-containing anticancer agents.Dalton transactions (Cambridge, England : 2003) · 2016Article
- Cellular Recognition and Repair of Monofunctional-Intercalative Platinum--DNA Adducts.Chemical research in toxicology · 2015Article
- Redesigning the DNA-targeted chromophore in platinum-acridine anticancer agents: a structure-activity relationship study.Chemistry (Weinheim an der Bergstrasse, Germany) · 2014Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
Using a versatile synthetic approach, a new class of potential ester prodrugs of highly potent, but systemically too toxic, platinum-acridine anticancer agents was generated. The new hybrids contain a hydroxyl group, which has been masked with a cleavable lipophilic acyl moiety. Both butanoic (butyric) and bulkier 2-propanepentanoic (valproic) esters were introduced. The goals of this design were to improve the drug-like properties (e.g., logD) and to reduce the systemic toxicity of the pharmacophore. Two distinct pathways by which the target compounds undergo effective ester hydrolysis, the proposed activating step, have been confirmed: platinum-assisted, self-immolative ester cleavage in a low-chloride environment (LC-ESMS, NMR spectroscopy) and enzymatic cleavage by human carboxylesterase-2 (hCES-2) (LC-ESMS). The valproic acid ester derivatives are the first example of a metal-containing agent cleavable by the prodrug-converting enzyme. They show excellent chemical stability and reduced systemic toxicity. Preliminary results from screening in lung adenocarcinoma cell lines (A549, NCI-H1435) suggest that the mechanism of the valproic esters may involve intracellular deesterification.
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Registered trials
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