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A new series of derivatives (compounds  8 – 20 ) of the breast antihormonal drug letrozole tagged with additional aryl groups were synthesized starting from the letrozole analog  7  via Suzuki cross-coupling reaction. Treatment of the ketone  9  with various aldehydes in base afforded the chalcone analogs  21 – 27 . The structural assignments were done by IR,  1 H,  13 C and 2D NMR spectra. Compounds  13 ,  21 – 23 ,  25  and  26  have been selected for their anticancer activity against MCF-7 and WRL-68 cell lines. Compounds  13  and  22  were found to be the most potent anticancer agents with IC 50  values of 34.75 and 58.79 (μg mL −1 ) (SI = 3.3 and 2.6, respectively). Molecular docking study of compounds  13  and  22  revealed hydrogen bond with the amino acids Arg115, Met374 and Met364 residues of the receptor 3EQM, respectively. Therefore, compounds  13  and  22  can be considered as promising anticancer agents due to their potent cytotoxic activity.

Design, synthesis, and in-silico study of new letrozole derivatives as prospective anticancer and antioxidant agents