5990-01-2Relevant academic research and scientific papers
Synthesis and biological evaluation of 1-phenyl-1,2,3,4-dihydroisoquinoline compounds as tubulin polymerization inhibitors
Zheng, Can-Hui,Chen, Jun,Liu, Jia,Zhou, Xiao-Tian,Liu, Na,Shi, Duo,Huang, Jing-Jing,Lv, Jia-Guo,Zhu, Ju,Zhou, You-Jun
, p. 454 - 462 (2012/08/28)
A series of 1-phenyl-3,4-dihydroisoquinoline derivatives and several 1-phenyl-1,2,3,4-tetrahydroisoquinoline, 1-phenyl-isoquinoline analogues were synthesized, and their cytotoxicity and tubulin polymerization inhibitory activity were evaluated. The 1-phenyl-3,4-dihydroisoquinoline compounds were found to be potential tubulin polymerization inhibitors. Compound 5n, bearing a 3′-OH and 4′-OCH3 substituted 1-phenyl B-ring, was shown to confer optimal bioactivity. The single-crystal structure of 5n was further determined by X-ray diffraction, and the binding mode of 5n to tubulin was obtained by molecular docking, which can explain the structure-activity relationships. The studies presented here provide a new structural type for the development of novel antitumor agents.
