Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.
Antineoplastic Agents; Carbazoles; Cell Line, Tumor; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Glioblastoma; Humans; Microtubules; Molecular Docking Simulation; Molecular Structure; Structure-Activity Relationship; Carbazole; Colchicine; Gliomas; Microtubules
Small molecules that target microtubules (MTs) represent promising therapeutics to treat certain types of cancer, including glioblastoma multiform (GBM). We synthesized modified carbazoles and evaluated their antitumor activity in GBM cells in culture. Modified carbazoles with an ethyl moiety linked to the nitrogen of the carbazole and a carbonyl moiety linked to distinct biaromatic rings exhibited remarkably different killing activities in human GBM cell lines and patient-derived GBM cells, with IC
Neurosciences (Brain & Spine)
Diaz, Philippe; Horne, Eric; Xu, Cong; Hamel, Ernest; Wagenbach, Michael; Petrov, Ravil R; Uhlenbruck, Benjamin; Haas, Brian; Hothi, Parvinder; Wordeman, Linda; Gussio, Rick; and Stella, Nephi, "Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells." (2018). Articles, Abstracts, and Reports. 809.