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Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors. | LitMetric

AI Article Synopsis

  • New histone deacetylase inhibitors have been developed and tested on the H661 non-small cell lung cancer cell line.
  • These inhibitors feature specially designed cyclic structures and a side chain that enhances their effectiveness.
  • The results showed that variants of these benzodiazepine-based compounds with specific aromatic groups had strong potential to inhibit cancer cell growth and target HDAC activity.

Article Abstract

New histone deacetylase inhibitors have been synthesized and evaluated for their activity against non-small lung cancer cell line H661. These compounds have been designed with diversely substituted 1,4-benzodiazepine-2,5-dione moieties as cyclic peptide mimic cap structures, and a hydroxamate side chain. Biological evaluations demonstrated that benzodiazepine-based HDACi bearing an aromatic substituent at the N1 position exhibited promising antiproliferative and HDAC-inhibitory activities.

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Source
http://dx.doi.org/10.1016/j.bmcl.2007.06.067DOI Listing

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