ArticleMolecular diversity2022
Itaconic acid hybrids as potential anticancer agents.
Article in Molecular diversity, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Itaconate and its derivatives in human health and diseases.Signal transduction and targeted therapy · 2026Review
- Biological and Teratogenic Evaluations of Nitrogen Heterocycles for Anticancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Synthesis and Characterization of Bioactive Oligoitaconates with Amino Acid Functional Groups for Tissue Engineering.International journal of molecular sciences · 2025Article
- Towards Greener Polymers: Poly(octamethylene itaconate-Polymers · 2025Article
- Novel and repurposed antiviral molecules for arbovirus infections with epidemic Potential: A systematic review.New microbes and new infections · 2025Review
- Enhanced Synthesis of Poly(1,4-butanediol itaconate) via Box-Behnken Design Optimization.Polymers · 2024Article
- Hydroxyhexylitaconic acids as potent IMP-type metallo-β-lactamase inhibitors for controlling carbapenem resistance inMicrobiology spectrum · 2024Article
- Photoclick reaction for rapid and simple fluorescence detection of itaconic acid and its derivatives in fungal cultures.Analytical and bioanalytical chemistry · 2023Article
- Recent Advances in Biotechnological Itaconic Acid Production, and Application for a Sustainable Approach.Polymers · 2021Review
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
In this paper, we report the synthesis of novel hybrids 2-14 based on itaconic acid and fluoroaniline, pyridine, indole and quinoline scaffolds. Itaconic acid is a naturally occurring compound with a Michael acceptor moiety, a key structural feature in several anticancer and antiviral drugs, responsible for the covalent binding of a drug to the cysteine residue of a specific protein. Aromatic parts of the hybrids also come from the substances reported as anticancer or antiviral agents. The synthetic route employed to access the amido-ester hybrids 2-13 used monomethyl itaconate or monomethyl itaconyl chloride and corresponding amines as the starting materials. Dimers 14 and 15 with two aminoindole or mefloquine moieties were prepared from itaconic acid and corresponding amino derivative, using standard coupling conditions (HATU/DIEA). All hybrids exerted anticancer effects in vitro against almost all the tumour cell lines that were evaluated (MCF-7, HCT 116, H460, LN-229, Capan-1, DND-41, HL-60, K-562, Z-138). Solid tumour cells were, in general, more responsive than the haematological cancer cells. The MCF-7 breast adenocarcinoma cell line appeared the most sensitive. Amido-ester 12 with chloroquine core and mefloquine homodimer 15 showed the highest activity with GI
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