scholarly journals Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphomain vitroandin vivo

Oncotarget ◽  
2014 ◽  
Vol 6 (7) ◽  
pp. 4976-4991 ◽  
Author(s):  
Han-Li Huang ◽  
Chieh-Yu Peng ◽  
Mei-Jung Lai ◽  
Chun-Han Chen ◽  
Hsueh-Yun Lee ◽  
...  
Keyword(s):  
B Cell ◽  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Histone Deacetylase Inhibitor ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Deacetylase Inhibitor ◽  
Potent Growth ◽  
Human B Cell

Inhibition of human B-cell development into plasmablasts by histone deacetylase inhibitor valproic acid

2013 ◽  
Vol 131 (6) ◽  
pp. 1695-1699.e9 ◽  
Author(s):  
Anne-Kathrin Kienzler ◽  
Marta Rizzi ◽  
Maike Reith ◽  
Stephen L. Nutt ◽  
Hermann Eibel
Keyword(s):  
Valproic Acid ◽  
B Cell ◽  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitor ◽  
Cell Development ◽  
B Cell Development ◽  
Deacetylase Inhibitor ◽  
Human B Cell

scholarly journals New Humulenes from Hyptis incana (Labiatae)

2013 ◽  
Vol 8 (12) ◽  
pp. 1934578X1300801
Author(s):  
Mitsuru Satoh ◽  
Yoshio Satoh ◽  
Yasuhiro Anzai ◽  
Daisuke Ajisawa ◽  
Keiichi Matsuzaki ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
Leukemia Cells ◽  
Moderate Activity ◽  
Mouse Leukemia ◽  
Aerial Parts ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Potent Growth

Two new humulene-type sesquiterpenes, named hyptishumulene I (1) and II (2), have been isolated, together with eight known compounds, a humulene-type sesquiterpene (3), a monoterpene (4) and six abietane-type diterpenoids (5–10) from the aerial parts of Hyptis incana (Labiatae). The cytotoxic activity of the isolated compounds against mouse leukemia cells (L1210) was examined. The abietane-type diterpenoids (5–10) showed rather potent growth inhibitory activity (IC50<15 μM), while the new humulene-type compounds (1 and 2) exhibited moderate activity (IC50>50 μM).

Synthesis of New β-Lactam Analogs and Evaluation of Their Histone Deacetylase (HDAC) Activity

2007 ◽  
Vol 62 (11) ◽  
pp. 1459-1464 ◽  
Author(s):  
Seikwan Oh ◽  
Jae-Chul Jung ◽  
Mitchell A. Avery
Keyword(s):  
Histone Deacetylase ◽  
Hdac Inhibitors ◽  
Human Tumor ◽  
Coupling Reactions ◽  
Human Tumor Cell Lines ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Potent Growth ◽  
High Yields

A simple synthesis of the β -lactams 11 - 13 and 16 - 17 as novel histone deacetylase (HDAC) inhibitors is described. The key synthetic strategies involved the O-alkylation of 6-APA and the coupling reactions of freshly prepared N-carbobenzyloxy-L-prolines 5 and 6 and 6-aminopenicillanates 8 - 10 and 15 in high yields. It was found that all compounds show potent growth inhibitory activity on human tumor cell lines, the most potent compound 16 exhibiting an IC50 = 2.1 μM in vitro.

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