ArticleScientific reports2018
High-affinity ligands of the colchicine domain in tubulin based on a structure-guided design.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed.
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Review
- Unraveling the mechanisms of benzimidazole resistance in hookworms: A molecular docking and dynamics study.Journal, genetic engineering & biotechnology · 2025Article
- Benzimidazole resistance-associated mutations improve theVeterinary world · 2024Article
- Synthesis,RSC medicinal chemistry · 2024Article
- PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.Journal of medicinal chemistry · 2024Article
- Article
- Frentizole, a Nontoxic Immunosuppressive Drug, and Its Analogs Display Antitumor Activity via Tubulin Inhibition.International journal of molecular sciences · 2023Article
- Exploring Pyrrolo-Fused Heterocycles as Promising Anticancer Agents: An Integrated Synthetic, Biological, and Computational Approach.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Docking experiments suggest that gloriosine has microtubule-targeting properties similar to colchicine.Scientific reports · 2023Article
- Article
- Quantification of Engagement of Microtubules by Small Molecules in Living Cells by Flow Cytometry.ACS bio & med chem Au · 2022Article
- pH-sensitive nanomedicine of novel tubulin polymerization inhibitor for lung metastatic melanoma.Journal of controlled release : official journal of the Controlled Release Society · 2022Article
- Identification of key interactions of benzimidazole resistance-associated amino acid mutations in Ascaris β-tubulins by molecular docking simulations.Scientific reports · 2022Article
- Hybridization Approach to Identify Salicylanilides as Inhibitors of Tubulin Polymerization and Signal Transducers and Activators of Transcription 3 (STAT3).Pharmaceuticals (Basel, Switzerland) · 2022Article
- Unveiling the Possible Oryzalin-Binding Site in the α-Tubulin ofACS omega · 2022Article
- Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective.Drug discovery today · 2022Review
- X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.Journal of medicinal chemistry · 2021Article
- New Estrone Oxime Derivatives: Synthesis, Cytotoxic Evaluation and Docking Studies.Molecules (Basel, Switzerland) · 2021Article
- Article
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Microtubule-targeting agents that bind at the colchicine-site of tubulin are of particular interest in antitumoral therapy due to their dual mechanism of action as antimitotics and vascular disrupting agents. Cyclohexanediones derivatives have been described as a new family of colchicine-domain binders with an association constant to tubulin similar to that of colchicine. Here, the high-resolution structures of tubulin in complex with cyclohexanediones TUB015 and TUB075 were solved by X-ray crystallography. A detailed analysis of the tubulin-TUB075 interaction by means of computational affinity maps allowed the identification of two additional regions at the binding site that were addressed with the design and synthesis of a new series of cyclohexanediones with a distal 2-substituted benzofurane. These new compounds showed potent antiproliferative activity with IC
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