ArticleEuropean journal of medicinal chemistry2018
2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
Article in European journal of medicinal chemistry, 2018. 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, 21 citations in OpenAlex.
- Synthesis and Antiproliferative Activity against Melanoma Cells of New Heterocyclic Hybrids Based on Pyridine and Pyrimidine Scaffolds.Current medicinal chemistry · 2026Article
- Discovery of a novel potent tubulin inhibitor through virtual screening and target validation for cancer chemotherapy.Cell death discovery · 2025Article
- Tubulin inhibitors: an insight into new strategies to combat leukemia.Future medicinal chemistry · 2025Review
- Article
- First total synthesis, antitumor evaluation and target identification of mornaphthoate E: A new tubulin inhibitor template acting on PI3K/Akt signaling pathway.Acta pharmaceutica Sinica. B · 2024Article
- Glochidiol, a natural triterpenoid, exerts its anti-cancer effects by targeting the colchicine binding site of tubulin.Investigational new drugs · 2021Article
- Synthesis and Anticancer Activity of Mitotic-Specific 3,4-Dihydropyridine-2(1International journal of molecular sciences · 2021Article
- Synthesis of aryl-substituted thieno[3,2-Beilstein journal of organic chemistry · 2019Article
Corrections and comments
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Authors and funding
15 authors at 6 institutions in 5 countries.
Funding
Abstract
Microtubules are recognized as crucial components of the mitotic spindle during cell division, and, for this reason, the microtubule system is an attractive target for the development of anticancer agents. Continuing our search strategy for novel tubulin targeting-compounds, a new series of 2-alkoxycarbonyl-3-(3',4',5'-trimethoxyanilino)-5-aryl/heteroarylthiophene derivatives was designed, synthesized and demonstrated to act as tubulin polymerization inhibitors at the colchicine site. A structure-activity relationship study on the phenyl at the 5-position of the thiophene ring was performed by introducing a variety of substituents containing electron-releasing and electron-withdrawing groups, with the 2-alkoxycarbonyl-3-(3',4',5'-trimethoxyanilino)thiophene scaffold being the minimum structural requirement for activity. Of the tested compounds, derivatives 4a, 4c, 4i and 4k possessed the highest overall potency and displayed high antiproliferative activities at submicromolar concentrations, with IC
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Registered trials
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