Design, synthesis and anticancer activities of halogenated Phenstatin analogs as microtubule destabilizing agent
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A series of halogenated Phenstatin analogs were designed as microtubule destabilizing agent by docking study. It was synthesized within three steps starting from 2-chloro-5-iodobenzoic acid and substituted benzene. All the products were characterized by 1H NMR and 13C NMR spectral analysis, and the stereochemical structure was also confirmed by a single crystal X-ray diffraction crystallographic analysis. The microtubule destabilizing activities were evaluated in vitro with human liver cancer Huh-7 cell line and human lung cancer A549 cell line. Some of the HPAs were achieved IC50 about 5.0 μM against human liver cancer Huh-7 cells.
KeywordsPhenstatin analogs Microtubule destabilizing agent Docking Anticancer CCK-8
We are grateful for the financial support from 2015 Beijing Natural Science Foundation (No. KZ201510005007) and thank professor Honggen Wang in Nankai University for single crystal X-ray diffraction technical assistance.
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Conflict of interest
The authors declare that they have no conflict of interest.
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