Synthesis and SAR requirements of adamantane–colchicine conjugates with both microtubule depolymerizing and tubulin clustering activities

ON Zefirova, EV Nurieva, DV Shishov, II Baskin…

文献索引：Zefirova, Olga N.; Nurieva, Evgeniya V.; Shishov, Dmitrii V.; Baskin, Igor I.; Fuchs, Fabian; Lemcke, Heiko; Schroeder, Fabian; Weiss, Dieter G.; Zefirov, Nikolay S.; Kuznetsov, Sergei A. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5529 - 5538

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被引用次数: 20

摘要

A series of analogues of conjugate 1, combining an adamantane-based paclitaxel (taxol) mimetic with colchicine was synthesized and tested for cytotoxicity in a cell-based assay with the human lung carcinoma cell line A549. The most active compounds (10 EC50 2±1.0 nM, 23 EC50 6±1.4 nM, 26 EC50 5±1.8 nM, 28 EC50 11±1.7 nM, 30 EC50 4.8±0.5 nM) were found to interfere with the microtubule dynamics in an interesting manner. Treatment of the ...