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.
Keywords: Synergistic effect, anti-proliferation, SAHA-based inhibitors, Cisplatin, hydroxamic acids.
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