A facile and atom-economical boric acid catalyzed direct amidation without any coupling
agents for the preparation of Suberoylanilide Hydroxamic Acid (SAHA) and SAHA-based inhibitors
targeting anti-proliferation of cancer cells is described. It is applicable to the preparation of SAHAbased
inhibitors having an unprotected hydroxyl group in the phenyl ring without the need of the protection.
The in-vitro assays data indicate that the nature and the position of the substituents (activating
and/or deactivating) in the capping group (phenyl ring) of SAHA-based inhibitors synthesized in this
study have a vital impact on the potency of anti-proliferative activity against cancer cells. With low toxicity toward the
normal cells, a number of synthesized SAHA-based inhibitors with two substituents in the phenyl ring possess higher antiproliferative
activity than SAHA and Cisplatin toward six studied cancer cell lines: A375 human skin cancer cells, A549
human lung cancer cells, MGC80-3 human gastric cancer cells, H460 human lung cancer cells, H1299 human lung cancer
cells, and HepG2 human liver cancer cells. Cisplatin is a common chemotherapeutic drug with high cytotoxicity for a variety
of cancer treatments. The inhibitors provided in this study might signify future therapeutic drugs for cancer
Keywords: Boric acid, SAHA-based inhibitors, anti-proliferation, Cisplatin, hydroxamic acid.
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