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Hydroxamic Acid Derivatives of Mycophenolic Acid Inhibit Histone Deacetylase at the Cellular Level
BATOVSKA, Daniela I.,KIM, Dong Hoon,MITSUHASHI, Shinya,CHO, Yoon Sun,KWON, Ho Jeong,UBUKATA, Makoto Japan Society for Bioscience, Biotechnology, and A 2008 Bioscience, biotechnology, and biochemistry Vol.72 No.10
<P>Mycophenolic acid (MPA, <B>1</B>), an inhibitor of IMP-dehydrogenase (IMPDH) and a latent PPARγ agonist, is used as an effective immunosuppressant for clinical transplantation and recently entered clinical trials in advanced multiple myeloma patients. On the other hand, suberoylanilide hydroxamic acid (SAHA), a non-specific histone deacetylase (HDAC) inhibitor, has been approved for treating cutaneous T-cell lymphoma. MPA seemed to bear a cap, a linker, and a weak metal-binding site as a latent inhibitor of HDAC. Therefore, the hydroxamic acid derivatives of mycophenolic acid having an effective metal-binding site, mycophenolic hydroxamic acid (MPHA, <B>2</B>), 7-<I>O</I>-acetyl mycophenolic acid (7-<I>O</I>-Ac MPHA, <B>3</B>), and 7-<I>O</I>-lauroyl mycophenolic hydroxamic acid (7-<I>O</I>-L MPHA, <B>4</B>) were designed and synthesized. All these compounds inhibited histone deacetylase with IC<SUB>50</SUB> values of 1, 0.9 and 0.5 μ<SMALL>M</SMALL>, and cell proliferation at concentrations of 2, 1.5 and 1 μ<SMALL>M</SMALL>, respectively.</P>