Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group
Psammaplin A (PsA) is a bromotyrosine disulfide dimer with histone deacetylase (HDAC) inhibition and acts through reduced monomer PsA-SH. We studied the connection of HDAC inhibition, cell growth inhibition, and apoptosis induction of PsA-SH by modifying the -SH group with deletion (6a) or replacement with hydroxamic acid (10b) or benzamide (12g). PsA-SH inhibits HDAC1/2/3 and 6a loses the HDAC inhibition ability. 10b inhibits HDAC1/2/3/6 while 12g shows selective inhibition of HDAC3. PsA-SH and 10b, but neither 6a nor 12g, induce apoptosis in human leukemia HL-60 cells associated with increased acetylation of Histone H3. PsA-SH and 10b inhibit growth of several solid tumor cell lines in vitro and Lewis lung cancer cell growth in vivo. PsA-SH is a simple scaffold for developing selective HDAC inhibitors and induces apoptosis through inhibiting HDAC1/2.
The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and us
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Page/Page column 70-71
(2008/06/13)
Electro-organic synthesis of N-hexyl carbamate by carbonylation of methanol and hexylamine with CO over Au supported on carbon anode
It has been found that Au anode, [AuBr3/AC+VGCF], showed the electro-catalysis for carbonylation of methanol, hexylamine and CO to 6-amino-hexyl-carbamic acid methyl ester (N-hexyl carbamate) using LiBr electrolyte.
De Leon, Roberto G.,Yamanaka, Ichiro,Otsuka, Kiyoshi
p. 764 - 765
(2007/10/03)
Reduction of Aliphatic and Aromatic Nitro Compounds with Sodium Borohydride in Tetrahydrofuran Using 10percent Palladium-on-Carbon as Catalyst
Aliphatic and aromatic nitro compounds are reduced to amino compounds in good yields with sodium borohydride in tetrahydrofuran using 10percent palladium-on-carbon as catalyst.
Petrini, Marino,Ballini, Roberto,Rosini, Goffredo
p. 713 - 714
(2007/10/02)
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