Design, synthesis, and antitumor evaluation of quinazoline-4-tetrahydroquinoline chemotypes as novel tubulin polymerization inhibitors targeting the colchicine site

We designed, synthesized, and evaluated the antitumor activity of a series of novel quinazoline-4-(6-methoxytetrahydroquinoline) analogues. Among the tested compounds, 4a4 exhibited the most potent antiproliferative activities across four human cancer cell lines with half-maximal inhibitory concentr...

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Veröffentlicht in:	European journal of medicinal chemistry 2025-02, Vol.283, p.117139, Article 117139
Hauptverfasser:	Lai, Qinhuai, Wang, Zhijia, Wu, Chengyong, Zhang, Ruofei, Li, Leyan, Tao, Yiran, Mo, Dan, Zhang, Jifa, Gou, Lantu, Wang, Yuxi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antitumor Apoptosis - drug effects Binding Sites Cell Line, Tumor Cell Proliferation - drug effects Co-crystal structure Colchicine - chemistry Colchicine - metabolism Colchicine - pharmacology Colchicine binding site inhibitors (CBSIs) Dose-Response Relationship, Drug Drug Design Drug Screening Assays, Antitumor Female Humans Mice Models, Molecular Molecular Structure Polymerization - drug effects Quinazoline-4-tetrahydroquinoline Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Quinolines - chemical synthesis Quinolines - chemistry Quinolines - pharmacology Structure-Activity Relationship Structure-activity relationship (SAR) Tubulin Tubulin - metabolism Tubulin Modulators - chemical synthesis Tubulin Modulators - chemistry Tubulin Modulators - pharmacology
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