Design, synthesis and bioevaluation of 2,7-diaryl-pyrazolo[1,5-a]pyrimidines as tubulin polymerization inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105220
Abstract: Two series of 2,7-diaryl-pyrazolo[1,5-a]pyrimidines as tubulin polymerization inhibitors were designed to restrict bioactive configuration of (E,Z)-vinylogous CA-4. All of the target compounds were synthesized and then evaluated for their in vitro antiproliferative activities against three… read more here.
Keywords: polymerization; polymerization inhibitors; pyrazolo pyrimidines; diaryl pyrazolo ... See more keywords
Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112716
Abstract: A series of novel vinyl selenone derivatives were designed, synthesized and evaluated as the tubulin polymerization inhibitors using a bioisosteric strategy. Among them, the representative compound 11k exhibited satisfactory anti-proliferative activities with IC50 values ranging… read more here.
Keywords: polymerization; polymerization inhibitors; microtubule polymerization; selenone derivatives ... See more keywords
Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113316
Abstract: A series of novel N-benzylbenzamide derivatives were designed and synthesized as tubulin polymerization inhibitors. Among fifty-one target compounds, compound 20b exhibited significant antiproliferative activities with IC50 values ranging from 12 to 27 nM against several cancer… read more here.
Keywords: polymerization inhibitors; novel benzylbenzamide; tubulin polymerization; discovery novel ... See more keywords
Discovery of Novel Acridane-Based Tubulin Polymerization Inhibitors with Anticancer and Potential Immunomodulatory Effects.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01566
Abstract: A series of novel acridane-based tubulin polymerization inhibitors were designed, synthesized, and bioevaluated as anticancer agents. The most potent compound NT-6 exhibited high tubulin polymerization inhibitory activity (IC50 = 1.5 μM) and remarkable antiproliferative potency… read more here.
Keywords: polymerization inhibitors; based tubulin; tubulin polymerization; acridane based ... See more keywords
Parvifoline Derivatives as Tubulin Polymerization Inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of natural products"
DOI: 10.1021/acs.jnatprod.8b00860
Abstract: A series of functionalized sesquiterpenoids derived from benzocyclooctene, including natural parvifoline (1), isoparvifoline (3), epoxyparvifoline (5), epoxyisoparvifoline (7), 8,12-oxyparfivoline (9), 8,14-oxyparvifoline (11), and the respective benzoyl derivatives 2, 4, 6, 8, 10, and 12, were… read more here.
Keywords: polymerization; polymerization inhibitors; derivatives tubulin; tubulin polymerization ... See more keywords
Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c05077
Abstract: A new series of 2,4-disubstituted thiazole derivatives containing 4-(3,4,5-trimethoxyphenyl) moiety was synthesized and evaluated for their potential anticancer activity as tubulin polymerization inhibitors. All designed compounds were screened for cytotoxic activity against four human cancer… read more here.
Keywords: molecular docking; polymerization inhibitors; thiazole derivatives; activity ... See more keywords
Biological activity and interaction mechanism of the diketopiperazine derivatives as tubulin polymerization inhibitors
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DOI: 10.1039/c7ra12173c
Abstract: Microtubules are a favorable target for development of anticancer agents. In this study, the anti-proliferative activities of plinabulin and six diketopiperazine derivatives were evaluated against human lung cancer cell line NCI-H460 and human pancreatic cancer… read more here.
Keywords: polymerization; polymerization inhibitors; diketopiperazine derivatives; derivatives tubulin ... See more keywords
Design, synthesis and biological evaluation of 9-aryl-5H-pyrido[4,3-b]indole derivatives as potential tubulin polymerization inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2022.1004835
Abstract: A series of new 9-aryl-5H-pyrido[4,3-b]indole derivatives as tubulin polymerization inhibitors were designed, synthesized, and evaluated for antitumor activity. All newly prepared compounds were tested for their anti-proliferative activity in vitro against three different cancer cells… read more here.
Keywords: tubulin polymerization; polymerization inhibitors; indole derivatives; aryl pyrido ... See more keywords