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.

Natural Compounds with Cell Growth Inhibitory Activity in Human Tumor Cell Lines

2013 ◽  
Vol 13 (10) ◽  
pp. 1582-1589 ◽  
Author(s):  
Cristiane Cazal ◽  
Kantima Choosang ◽  
Vanessa Severino ◽  
João Fernandes ◽  
Maria Silva ◽  
...  
Keyword(s):  
Cell Growth ◽  
Tumor Cell ◽  
Cell Lines ◽  
Inhibitory Activity ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity

scholarly journals Purification and characterization of a novel monocyte chemotactic and activating factor produced by a human myelomonocytic cell line.

1989 ◽  
Vol 169 (4) ◽  
pp. 1485-1490 ◽  
Author(s):  
K Matsushima ◽  
C G Larsen ◽  
G C DuBois ◽  
J J Oppenheim
Keyword(s):  
Cell Line ◽  
Human Tumor ◽  
Heparin Binding ◽  
Purification And Characterization ◽  
Human Tumor Cell Lines ◽  
Growth Inhibitory ◽  
Sds Page ◽  
Normal Human

A novel basic heparin-binding monocyte chemotactic factor (MCF) was purified to homogeneity from the conditioned media of human myelomonocytic cell line THP-1 based on its in vitro monocyte chemotactic activity. The purified MCF was homogenous and estimated to be 15 kD on SDS-PAGE. Purified MCF stimulated normal human monocytes to be growth inhibitory in vitro at 2-3 d for several human tumor cell lines. This represents the first report of the identification and purification of a chemoattractant cytokine that also activates monocytes but is distinct from interferons and other known cytokines.

scholarly journals Sartoryglabrins, Analogs of Ardeemins, from Neosartorya Glabra

2011 ◽  
Vol 6 (6) ◽  
pp. 1934578X1100600
Author(s):  
Anake Kijjoa ◽  
Sonia Santos ◽  
Tida Dethoup ◽  
Leka Manoch ◽  
Ana Paula Almeida ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Human Tumor ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Growth Inhibitory ◽  
Nmr Spectrometry ◽  
Growth Inhibitory Activity ◽  
Mcf 7

Chemical investigation of a collection of the fungus Neosartorya glabra from Thailand furnished sartoryglabins A-C (1a, 1b and 2) which are analogs of the reverse prenylated indole alkaloids known as (-) ardeemins. Structures of these compounds were established by NMR spectrometry and an X-ray analysis. Sartoryglabins A-C were evaluated for their in vitro growth inhibitory activity on three human tumor cell lines: MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and A375-C5 (melanoma). All the compounds exhibited strong to moderate activity against the MCF-7 cell line but weak or no activity against the NCI-H460 and A375-C5 cell lines. Sartoryglabin B was found to exhibit selectivity towards the MCF-7 cell line.

Sign in / Sign up

Export Citation Format

Share Document