Triazolo‐linked benzimidazoles as tubulin polymerization inhibitors and DNA intercalators: Design, synthesis, cytotoxicity, and docking studies
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200449
Abstract: A simple “click” protocol was employed in the quest of synthesizing 1,2,3‐triazole‐linked benzimidazoles as promising anticancer agents on various human cancer cell lines such as A549, HCT116, SK‐Mel‐28, HT‐29, and MCF‐7. Compound 12j demonstrated significant… read more here.
Keywords: dna; cytotoxicity; docking studies; tubulin polymerization ... See more keywords
Design, Synthesis, and in vitro and in vivo Evaluations of (Z)‐3,4,5‐Trimethoxystyrylbenzenesulfonamides/sulfonates as Highly Potent Tubulin Polymerization Inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "ChemMedChem"
DOI: 10.1002/cmdc.201600643
Abstract: Newer therapeutics can be developed in drug discovery by adopting the strategy of scaffold hopping of the privileged scaffolds from known bioactive compounds. This strategy has been widely employed in drug‐discovery processes. Structure‐based docking studies… read more here.
Keywords: tubulin polymerization; synthesis vitro; polymerization; design synthesis ... See more keywords
9-Ethynyl noscapine induces G2/M arrest and apoptosis by disrupting tubulin polymerization in cervical cancer.
Sign Up to like & getrecommendations! Published in 2021 at "Drug development research"
DOI: 10.1002/ddr.21888
Abstract: Noscapine is a phthalide isoquinoline alkaloid present in the latex of Papaver somniferum and has demonstrated potent antitumor activity in various cancer models. Structural changes in the core molecule of noscapine architecture have produced a… read more here.
Keywords: apoptosis; cervical cancer; tubulin polymerization; cancer ... See more keywords
Identification of KX2‐391 as an inhibitor of HBV transcription by a recombinant HBV‐based screening assay
Sign Up to like & getrecommendations! Published in 2017 at "Antiviral Research"
DOI: 10.1016/j.antiviral.2017.06.005
Abstract: Abstract Antiviral therapies for chronic hepatitis B virus (HBV) infection that are currently applicable for clinical use are limited to nucleos(t)ide analogs targeting HBV polymerase activity and pegylated interferon alpha (PEG‐IFN). Towards establishing an effective… read more here.
Keywords: anti hbv; hbv; tubulin polymerization; recombinant hbv ... See more keywords
Synthesis and biological evaluation of new 2-methoxyestradiol derivatives: Potent inhibitors of angiogenesis and tubulin polymerization.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.104988
Abstract: Here, we report the structural optimization of a hit natural compound, 2-ME2 (2-methoxyestradiol), which exhibited inhibitory activity but low potency on tubulin polymerization, anti- angiogenesis, MCF-7 proliferation and metastasis in vitro and in vivo. A… read more here.
Keywords: methoxyestradiol; polymerization; proliferation metastasis; tubulin polymerization ... See more keywords
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
Synthesis and biological evaluation of indole-2-carbohydrazides and thiazolidinyl-indole-2-carboxamides as potent tubulin polymerization inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Computational biology and chemistry"
DOI: 10.1016/j.compbiolchem.2019.05.002
Abstract: A new series of N'-(substituted phenyl)-5-chloro/iodo-3-phenyl-1H-indole-2-carbohydrazide (5, 6) and N-[2-(substituted phenyl)-4-oxo-1,3-thiazolidin-3-yl]-5-iodo/chloro-3-phenyl-1H-indole-2-carboxamide (7, 8) derivatives were synthesized and evaluated for their anticancer properties. Compounds 5a and 6b, selected as prototypes by the National Cancer Institute for… read more here.
Keywords: synthesis biological; biological evaluation; evaluation indole; cancer ... See more keywords
Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.08.018
Abstract: A series of novel N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxy- lic acid derivatives were synthesized and evaluated for their biological activities. Among all synthesized target compounds, 13d exhibited the most potent antiproliferative activity against HeLa, SMMC-7721, K562 cell line (IC50 = 0.126 μM,… read more here.
Keywords: tetrahydro quinoxaline; tubulin polymerization; acid derivatives; oxo tetrahydro ... See more keywords
A class of novel tubulin polymerization inhibitors exert effective anti-tumor activity via mitotic catastrophe.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.12.030
Abstract: In current work, a class of novel 4,5-dihydro-1H-pyrazole-1-carboxylate derivatives (E01-E28) were designed, synthesized and evaluated. Among them, the most potent compound E24 exhibited comparable activity against a panel of cancer cells (GI50 ranging 0.05-0.98 μM) and… read more here.
Keywords: class novel; tubulin polymerization; tubulin; compound e24 ... See more keywords
Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111949
Abstract: A combination therapeutic regimen via introducing tryptophan 2,3-dioxygenase inhibitors into microtubule inhibitors was performed and evaluated for their antitumor activity. Thereinto, HT2, composed of combretastatin A-4 (CA-4) and tryptophan-2,3-dioxygenase (TDO) inhibitor by a linker, displayed… read more here.
Keywords: microtubule inhibitors; tubulin polymerization; tryptophan dioxygenase; cancer ... 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