ArticleCells2018
Synthesis and Biological Evaluation of Novel Triple-Modified Colchicine Derivatives as Potent Tubulin-Targeting Anticancer Agents.
Article in Cells, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 28 citations in OpenAlex.
- The therapeutic potential of colchicine in oncology studies: from structural modification and targeted delivery to clinical management.Frontiers in pharmacology · 2026Review
- Glycosaminoglycans Targeted by Colchicine in MCF-7 Cells.Pharmaceutics · 2025Article
- Design, synthesis and antiproliferative activity of novel colchicine derivatives: selective inhibition of melanoma cell proliferation.Frontiers in pharmacology · 2025Article
- Benzotriazole Substituted 2-Phenylquinazolines as Anticancer Agents: Synthesis, Screening, Antiproliferative and Tubulin Polymerization Inhibition Activity.Current cancer drug targets · 2023Article
- Changes in Key Aroma Compounds and Esterase Activity ofFoods (Basel, Switzerland) · 2022Article
- Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones.International journal of molecular sciences · 2022Review
- Article
- Synthesis and Antiproliferative Evaluation of 3-Chloroazetidin-2-ones with Antimitotic Activity: Heterocyclic Bridged Analogues of Combretastatin A-4.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Antiviral, Cytotoxic, and Antioxidant Activities of Three Edible Agaricomycetes Mushrooms:Journal of fungi (Basel, Switzerland) · 2021Article
- Status and Challenges of Plant-Anticancer Compounds in Cancer Treatment.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Mitotic Poisons in Research and Medicine.Molecules (Basel, Switzerland) · 2020Review
- Synthesis and Antiproliferative Screening Of Novel Analogs of Regioselectively Demethylated Colchicine and Thiocolchicine.Molecules (Basel, Switzerland) · 2020Article
- Metabolites of Vinca Alkaloid Vinblastine: Tubulin Binding and Activation of Nausea-Associated Receptors.ACS omega · 2019Article
- In silico study of colchicine resistance molecular mechanisms caused by tubulin structural polymorphism.PloS one · 2019Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 3 countries.
Funding
Abstract
Specific modifications of colchicine followed by synthesis of its analogues have been tested in vitro with the objective of lowering colchicine toxicity. Our previous studies have clearly shown the anticancer potential of double-modified colchicine derivatives in C-7 and C-10 positions. Here, a series of novel triple-modified colchicine derivatives is reported. They have been obtained following a four-step strategy. In vitro cytotoxicity of these compounds has been evaluated against four human tumor cell lines (A549, MCF-7, LoVo, and LoVo/DX). Additionally, the mode of binding of the synthesized compounds was evaluated in silico using molecular docking to a 3D structure of β-tubulin based on crystallographic data from the Protein Data Bank and homology methodology. Binding free energy estimates, binding poses, and MlogP values of the compounds were obtained. All triple-modified colchicine derivatives were shown to be active at nanomolar concentrations against three of the investigated cancer cell lines (A549, MCF-7, LoVo). Four of them also showed higher potency against tumor cells over normal cells as confirmed by their high selectivity index values. A vast majority of the synthesized derivatives exhibited several times higher cytotoxicity than colchicine, doxorubicin, and cisplatin.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.