Structure–activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium

The minimum structural requirements for troglitazone-like compounds to retain their biological activities were reported. Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-05, Vol.14 (10), p.2547-2550
Hauptverfasser: Fan, Yun-Hua, Chen, Han, Natarajan, Amarnath, Guo, Yuhong, Harbinski, Fred, Iyasere, Julia, Christ, William, Aktas, Huseyin, Halperin, Jose A.
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Sprache:eng
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Zusammenfassung:The minimum structural requirements for troglitazone-like compounds to retain their biological activities were reported. Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.02.087