Summary: | <div class="WordSection1"><p><em>Retinoids</em><em> are a class of natural and synthetic vitamin A analogues</em><em> structurally related to</em><em> all-trans-retinoic acid (ATRA). This class of compounds can inhibit cell proliferation and induce differentiation and apoptosis of cells, and several are used in cancer therapy. Using the concept of bioisosterism, new triazole analogues were designed from the molecular modification of the potent derivative arotinoid AM580. This compound has an amide grouping which is a </em><em>bioisostere</em><em> of 1,2,3-triazole ring. Through "Click Chemistry” approach, triazole analogues were obtained by reaction of Huisgen 1,3-dipolar cycloaddition between aryl azides and terminal acetylene, previously synthesized. The reagents used were CuI, triethylamine and mixture of ethanol:water. The first compound synthesized showed anticancer activity, while the second proved to be inactive. The molecular docking results showed that both compounds have high affinity for the retinoid RAR</em><em>α </em><em>receptor</em><em> (</em><em>related to anticancer activity), but probably the second compound has antagonist activity on this receptor.</em></p></div>
|