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Design, synthesis and anticancer activities of halogenated Phenstatin analogs as microtubule destabilizing agent

  • Shengquan Hu
  • Wuji Sun
  • Yeming Wang
  • Hong YanEmail author
Original Research
  • 34 Downloads

Abstract

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.

Keywords

Phenstatin analogs Microtubule destabilizing agent Docking Anticancer CCK-8 

Notes

Acknowledgements

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.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  1. 1.Beijing Key Laboratory of Environmental and Viral Oncology, College of Life Science and Bio-engineeringBeijing University of TechnologyBeijingChina
  2. 2.Beijing Tide Pharmaceutical Co., LtdBeijingChina

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