Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112323
Abstract: Inhibition of tubulin polymerisation with small molecules has been clinically validated as a promising therapy for multiple solid tumours. Herein, a series of chiral azetidin-2-ones were asymmetrically synthesised and biologically evaluated for antitumour activities. Among… read more here.
Keywords: tubulin polymerisation; azetidin one; fluorinated azetidin; chiral fluorinated ... See more keywords
Antiproliferative benzothiazoles incorporating a trimethoxyphenyl scaffold as novel colchicine site tubulin polymerisation inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2020.1753721
Abstract: Abstract Tubulin polymerisation inhibitors exhibited an important role in the treatment of patients with prostate cancer. Herein, we reported the medicinal chemistry efforts leading to a new series of benzothiazoles by a bioisosterism approach. Biological… read more here.
Keywords: chemistry; tubulin polymerisation; colchicine; site tubulin ... See more keywords
Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
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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
Synthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors
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DOI: 10.1080/14756366.2022.2122962
Abstract: Abstract A series of litseaone B analogues 4a∼4p were synthesised and antitumor activities of all compounds were screened. These compounds were designed by introducing different substituents on the B ring. Among these synthesised compounds, it… read more here.
Keywords: tubulin polymerisation; litseaone analogues; antitumor; activity ... See more keywords