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- W4285388775 abstract "Inhibition of histone deacetylases (HDACs) has been extensively studied in the development of anticancer drugs. In the discovery of potent HDAC inhibitors with novel structures, the 2-substituted phenylquinoline-4-carboxylic acid group was introduced to the cap moiety of HDAC inhibitors. In total, 30 compounds were synthesized with hydroxamic acid or hydrazide zinc-binding groups. In the enzyme inhibitory test, active compound D28 and its analog D29 exhibited significant HDAC3 selectivity against HDAC1, 2, 3, and 6. However, compared with D28 , the hydrazide-bearing compounds ( D29 and D30 ) with remarkably improved enzyme inhibitory activities did not exhibit significant antiproliferative potency in the in vitro anticancer study. Further K562 cell-based mechanistic results revealed that induction of G2/M cell cycle arrest and promotion of apoptosis make important contributions to the anticancer effects of molecule D28 . Collectively, an HDAC3 selective inhibitor ( D28 ) with potent in vitro anticancer activity was developed as a lead compound for the treatment of cancer." @default.
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- W4285388775 date "2022-07-14" @default.
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- W4285388775 title "Discovery of 2-Phenylquinoline-4-Carboxylic Acid Derivatives as Novel Histone Deacetylase Inhibitors" @default.
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- W4285388775 doi "https://doi.org/10.3389/fchem.2022.937225" @default.
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