Abstract
Abstract Retinoids, the derivatives of vitamin A, are known to exhibit anticancer properties through binding to nuclear retinoic acid receptors (RARs). However, several factors such as high lipophilicity, short half life, associated toxicity and appearance of resistant cells during differentiation therapy has limited their therapeutic potential. Here we report synthesis of aryl/heterocyclic analogs of retinoid trans-2-octenal with and without copper complexation. The biological activity of these novel synthetic compounds was tested against multiple human cancer cell lines: breast cancer cell lines MCF-7, BT-20, MDA-MB-231 and prostate cancer cell line PC-3, all of which differ in their expression of RAR subunits. The retinoid-derivatives were found to be effective in inhibiting the growth of all the cell lines, particularly those that express RAR α. Synthesis of hydrazonate analogs of retinoic acid and their copper conjugation is therefore an effective strategy to design novel anticancer compounds.
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