Rui Xie, Jinghua Shi, Chunhui Cheng, Fan Yun, Xia Liu, Pingwah Tang, Xinying Wu, Ming Yang and Qipeng Yuan Pages 767 - 774 ( 8 )
A novel, green, and atom-economical boric acid catalyzed direct amidation without the use of any coupling agents for the preparation of suberoylanilide hydroxamic acid (SAHA) and SAHA-based inhibitors targeting anti-proliferation of cancer cells is provided. The new SAHA-based inhibitor B123, when used alone, exhibited higher anti-proliferative activities than SAHA or Cisplatin against a number of human cancer cells. We have examined the effect of combination of these SAHA-based inhibitors with Cisplatin. We found synergistic effects of the combination of SAHA-based inhibitors with Cisplatin over a wide range of concentrations against human liver cancer cells HepG2 and two human lung cancer cell lines H1299 and H460. This synergism leads up to 8-fold of dose reduction for Cisplatin in the combination with our synthesized inhibitor B123 against H1299.
Synergistic effect, anti-proliferation, SAHA-based inhibitors, Cisplatin, hydroxamic acids.
College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China.