| Literature DB >> 21420302 |
Hanae Benelkebir1, Sabrina Marie, Annette L Hayden, Jason Lyle, Paul M Loadman, Simon J Crabb, Graham Packham, A Ganesan.
Abstract
The total synthesis of largazole and four analogues is reported. All analogues were nanomolar HDAC inhibitors. The antiproliferative activity is driven by lipophilicity and cell permeability. In murine liver homogenates, largazole is rapidly metabolized (half-life ≤5 min) to the thiol which has a half-life of 51 min.Entities:
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Year: 2011 PMID： 21420302 DOI： 10.1016/j.bmc.2011.02.024
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641