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Discovery of dual tubulin-NEDDylation inhibitors with antiproliferative activity.
Publication Type: Academic Journal
Source(s): Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2023 Dec; Vol. 38 (1), pp. 166-175.
Abstract: Although various dual-target tubulin inhibitors have been designed and synthesised, no dual tubulin-NEDDylation inhibitors as antiproliferative agents were reported so far. In this work, a series of trimethoxyphenyl analogues as potential dual tubulin-...
Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation.
Publication Type: Academic Journal
Source(s): Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2023 Dec; Vol. 38 (1), pp. 2155815.
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 vit...
Design, synthesis and biological evaluation of novel dihydroquinolin-4(1H)-one derivatives as novel tubulin polymerization inhibitors.
Publication Type: Academic Journal
Source(s): European journal of medicinal chemistry [Eur J Med Chem] 2023 Dec 15; Vol. 262, pp. 115881. Date of Electronic Publication: 2023 Oct 15.
Abstract: A series of novel dihydroquinolin-4(1H)-one derivatives targeting colchicine binding site on tubulin were designed, synthesized and evaluated as anticancer agents. The most potent compound 6t showed remarkable antiproliferative activities against four ...
Design, synthesis and evaluation of dihydro-1 H -indene derivatives as novel tubulin polymerisation inhibitors with anti-angiogenic and antitumor potency.
Publication Type: Academic Journal
Source(s): Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2023 Dec; Vol. 38 (1), pp. 2247579.
Abstract: Angiogenesis plays an important role in tumour generation and progression, which is used to supply nutrients and metastasis. Herein, a series of novel dihydro-1 H -indene derivatives were designed and evaluated as tubulin polymerisation inhibitors by b...
Discovery of novel arylamide derivatives containing piperazine moiety as inhibitors of tubulin polymerisation with potent liver cancer inhibitory activity.
Publication Type: Academic Journal
Source(s): Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2023 Dec; Vol. 38 (1), pp. 2237701.
Abstract: In this work, a series of novel arylamide derivatives containing piperazine moiety were designed and synthesised as tubulin polymerisation inhibitors. Among 25 target compounds, compound 16f ( MY-1121 ) exhibited low nanomolar IC 50 values ranging from...
Development of QTMP: A promising anticancer agent through NP-Privileged Motif-Driven structural modulation.
Publication Type: Academic Journal
Source(s): Bioorganic & medicinal chemistry [Bioorg Med Chem] 2023 Nov 15; Vol. 95, pp. 117489. Date of Electronic Publication: 2023 Oct 05.
Abstract: In this study of creating new molecules from clinical trial agents, an approach of Combretastatin structural modulation with the installation of NP-privileged motifs was considered, and a series of trimethoxyphenyl-2-aminoimidazole with functionalized ...
Benzimidazole derivatives as tubulin polymerization inhibitors: Design, synthesis and in vitro cytotoxicity studies.
Publication Type: Academic Journal
Source(s): Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2023 Nov 15; Vol. 96, pp. 129494. Date of Electronic Publication: 2023 Oct 03.
Abstract: A new class of benzimidazole derivatives as tubulin polymerization inhibitors has been designed and synthesized in this study. The in vitro anticancer profile of the developed molecules was reconnoitred on selected human cancer cells. The highest cytot...
Design, Synthesis, and Antitumor Efficacy of Substituted 2-Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2.
Publication Type: Academic Journal
Source(s): Journal of medicinal chemistry [J Med Chem] 2023 Nov 09; Vol. 66 (21), pp. 15006-15024. Date of Electronic Publication: 2023 Oct 19.
Abstract: Preclinical and clinical studies have demonstrated the synergistic effect of microtubule-targeting agents in combination with Janus kinase 2 (JAK2) inhibitors, prompting the development of single agents with enhanced therapeutic efficacy by dually inhi...
Design, synthesis, and biological evaluation of 3, 5-disubsituted-1H-pyrazolo[3,4-b]pyridines as multiacting inhibitors against microtubule and kinases.
Publication Type: Academic Journal
Source(s): European journal of medicinal chemistry [Eur J Med Chem] 2023 Nov 05; Vol. 259, pp. 115687. Date of Electronic Publication: 2023 Jul 27.
Abstract: Combination therapy of kinases inhibitors and chemotherapeutics targeting tubulin dynamics is an important strategy to improve therapeutic efficacy and overcome the resistance to single-target drug therapies. Inspired by this, we report herein the rati...
Design, synthesis and bioevaluation of novel trifluoromethylquinoline derivatives as tubulin polymerization inhibitors.
Publication Type: Academic Journal
Source(s): Future medicinal chemistry [Future Med Chem] 2023 Nov; Vol. 15 (21), pp. 1967-1986. Date of Electronic Publication: 2023 Nov 08.
Abstract: Aim: A series of novel trifluoromethylquinoline derivatives were designed, synthesized and evaluated for antitumor activities. Methodology: All compounds were evaluated for antiproliferative activity against four human cancer cell lines. Results: Among...