AI Article Synopsis
- A series of novel compounds called 2'-benzyloxy-5'-substituted-5-benzylidene-thiazolidine derivatives were created to find new inhibitors for translation initiation in cancer therapy.
- Several of these compounds, specifically 5-benzylidene-thiazolidine-2,4-diones and thiones, showed significant cell growth inhibition.
- The mechanism of action involves the depletion of calcium stores inside cells and increased phosphorylation of a protein called eIF2alpha, affecting translation initiation.
Article Abstract
In an effort to generate novel translation initiation inhibitors for cancer therapy, a series of 2'-benzyloxy-5'-substituted-5-benzylidene-thiazolidine-2,4-thione and dione derivatives was synthesized and evaluated for activity in translation initiation specific assays. Several candidates of the 5-benzylidene-thiazolidine-2,4-diones (3c, 3d, and 3f) and -thiones (2b, 2e, and 2j), inhibit cell growth with low microM GI(50) mediated by inhibition of translation initiation, which involves partial depletion of intracellular Ca(2+) stores and strong phosphorylation of eIF2alpha.
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| http://dx.doi.org/10.1016/j.bmcl.2004.08.017 | DOI Listing |
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