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Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.


ABSTRACT: Thujaplicins are tropolone-derived natural products with antiproliferative properties. We recently reported that certain tropolones potently and selectively target histone deacetylases (HDAC) and inhibit the growth of hematological cell lines. Here, we investigated the mechanisms by which these compounds exert their antiproliferative activity in comparison with the pan-selective HDAC inhibitor, vorinostat, using Jurkat T-cell leukemia cells. The tropolones appear to work through a mechanism distinct from vorinostat. These studies suggest that tropolone derivatives may serve as selective epigenetic modulators of hematological cells with potential applications as anti-leukemic or anti-inflammatory agents.

SUBMITTER: Ononye SN 

PROVIDER: S-EPMC4011186 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature

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Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.

Ononye Sophia N SN   Vanheyst Michael D MD   Giardina Charles C   Wright Dennis L DL   Anderson Amy C AC  

Bioorganic & medicinal chemistry 20140222 7


Thujaplicins are tropolone-derived natural products with antiproliferative properties. We recently reported that certain tropolones potently and selectively target histone deacetylases (HDAC) and inhibit the growth of hematological cell lines. Here, we investigated the mechanisms by which these compounds exert their antiproliferative activity in comparison with the pan-selective HDAC inhibitor, vorinostat, using Jurkat T-cell leukemia cells. The tropolones appear to work through a mechanism dist  ...[more]

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