Synthesis and Biological Investigation of Δ<sup>12</sup>-Prostaglandin J<sub>3</sub> (Δ<sup>12</sup>-PGJ<sub>3</sub>) Analogues and Related Compounds


A series of Δ<sup>12</sup>-prostaglandin J<sub>3</sub> (Δ<sup>12</sup>-PGJ<sub>3</sub>) analogues and derivatives were synthesized employing an array of synthetic strategies developed specifically to render them readily available for biological investigations. The synthesized compounds were evaluated for their cytotoxicity against a number of cancer cell lines, revealing nanomolar potencies for a number of them against certain cancer cell lines. Four analogues (<b>2</b>, <b>11</b>, <b>21</b>, and <b>27</b>) demonstrated inhibition of nuclear export through a covalent addition at Cys528 of the export receptor Crm1. One of these compounds (i.e., <b>11</b>) is currently under evaluation as a potential drug candidate for the treatment of certain types of cancer. These studies culminated in useful and path-pointing structure–activity relationships (SARs) that provide guidance for further improvements in the biological/pharmacological profiles of compounds within this class

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oai:figshare.com:article/3374041Last time updated on 2/12/2018

This paper was published in FigShare.

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