Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00715
Abstract: We previously reported a potent tubulin inhibitor CH-2-77. In this study, we optimized the structure of CH-2-77 by blocking metabolically labile sites and synthesized a series of CH-2-77 analogues. Two compounds, 40a and 60c, preserved… read more here.
Keywords: tubulin; binding site; colchicine binding; potential anticancer ... See more keywords
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.
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DOI: 10.1021/acs.jmedchem.2c01208
Abstract: Targeting the colchicine binding site on tubulin is a promising strategy to develop cancer therapeutics. Herein, we describe our systematic structure-activity relationship studies of benzamide derivatives that lead to an identification of a potent and… read more here.
Keywords: tubulin; benzamide derivatives; colchicine binding; targeting colchicine ... See more keywords
Design, Synthesis, and Biological Evaluation of Heterocyclic-Fused Pyrimidine Chemotypes Guided by X-ray Crystal Structure with Potential Antitumor and Anti-multidrug Resistance Efficacy Targeting the Colchicine Binding Site.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c02115
Abstract: Herein, a series of quinazoline and heterocyclic fused pyrimidine analogues were designed and synthesized based on the X-ray co-crystal structure of lead compound 3a, showing efficacious antitumor activities. Two analogues, 15 and 27a, exhibited favorable… read more here.
Keywords: antitumor; colchicine binding; heterocyclic fused; fused pyrimidine ... See more keywords
Novel quinolone chalcones targeting colchicine-binding pocket kill multidrug-resistant cancer cells by inhibiting tubulin activity and MRP1 function
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DOI: 10.1038/s41598-017-10972-0
Abstract: Agents targeting colchicine-binding pocket usually show a minimal drug-resistance issue, albeit often associated with high toxicity. Chalcone-based compounds, which may bind to colchicine-binding site, are found in many edible fruits, suggesting that they can be… read more here.
Keywords: binding pocket; colchicine binding; multidrug resistant; cancer cells ... See more keywords
Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2020.1783664
Abstract: Abstract Tubulin polymerisation inhibitors that target colchicine binding site were powerful anticancer agents. Although along the years many colchicine binding site inhibitors (CBSIs) have been reported, few piperidine derivatives were identified as CBSIs. In this… read more here.
Keywords: pc3 cells; binding site; piperidine derivatives; colchicine binding ... See more keywords
Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2021.1883598
Abstract: Abstract Discovering of new anticancer agents with potential activity against tubulin polymerisation is still a promising approach. Colchicine binding site inhibitors are the most relevant anti-tubulin polymerisation agents. Thus, new quinoline derivatives have been designed… read more here.
Keywords: site inhibitors; binding site; tubulin polymerisation; colchicine binding ... See more keywords
Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2155815
Abstract: Abstract The colchicine binding site of tubulin is a promising target for discovering novel antitumour agents. Previously, we identified 2-aryl-4-amide-quinoline derivatives displayed moderate tubulin polymerisation inhibitory activity and broad-spectrum in vitro antitumour activity. In this… read more here.
Keywords: binding site; colchicine binding; activity; tubulin ... See more keywords
Synthesis and Molecular Docking of Some Grossgemin Amino Derivatives as Tubulin Inhibitors Targeting Colchicine Binding Site
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DOI: 10.1155/2021/5586515
Abstract: Six amino derivatives of grossgemin (2–7) were synthesized according to the reported essential pharmacophoric features of colchicine binding site inhibitors (CBSIs). The derivatives 4–6 were obtained for the first time. The pharmacophoric features of 2–7… read more here.
Keywords: amino derivatives; binding site; colchicine binding; colchicine ... See more keywords
Abstract 3223: Novel tubulin inhibitor DJ101 targets the colchicine binding site and suppresses melanoma growth and metastasis
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DOI: 10.1158/1538-7445.am2017-3223
Abstract: Interfering with microtubule dynamics is a validated approach for anticancer treatment and by selectively targeting the colchicine binding site on tubulin, microtubule destabilizing agents can evade mechanisms of drug resistance that commonly develop with other… read more here.
Keywords: tubulin; binding site; tubulin inhibitor; colchicine binding ... See more keywords
Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy
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DOI: 10.3390/biom12121843
Abstract: Cancer accounts for numerous deaths each year, and it is one of the most common causes of death worldwide, despite many breakthroughs in the discovery of novel anticancer candidates. Each new year the FDA approves… read more here.
Keywords: binding site; tubulin inhibitors; colchicine binding; cancer ... See more keywords
An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors.
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DOI: 10.4155/fmc-2022-0212
Abstract: Microtubules, formed by α- and β-tubulin heterodimer, are considered as a major target to prevent the proliferation of tumor cells. Microtubule-targeted agents have become increasingly effective anticancer drugs. However, due to the relatively sophisticated chemical… read more here.
Keywords: discovery novel; colchicine binding; advances discovery; update recent ... See more keywords