Synthesis, characterization and anti-tumor activity of moxifloxacin–Copper complexes against breast cancer cell lines

Novel moxifloxacin–copper complexes were synthesized, characterized and screened for anti-proliferative and apoptosis-inducing activity against multiple human breast cancer cell lines (hormone-dependent MCF-7 and T47D as well as hormone-independent MDA-MB-231 and BT-20). The results indicated that the parent compound moxifloxacin (1) does not exert any inhibitory activity against breast cancer cell lines examined. On the other hand, the copper conjugate 2 and its nitrogen adducts 3–5 exerted growth inhibitory and apoptosis-inducing activity against breast cancer cell lines without any substantial effect on non-tumorigenic breast epithelial cells MCF-10A at equimolar concentration, suggesting a cancer cell-specific activity. BT-20 cells were more sensitive to compounds 2 and 3, while compounds 4 and 5 exerted significant anti-proliferative and apoptosis-inducing effects on T47D, MDA-MB-231 and BT-20 cell lines. Our results suggest that these novel compounds could be useful for the treatment of breast cancer in the future.

Graphical abstractNovel moxifloxacin–copper complexes were synthesized, characterized and screened for anti-proliferative and apoptosis-inducing activity against hormone dependent (MCF-7 and T47D) and hormone independent (MDA-MB-231 and BT-20) breast cancer cell lines and was compared against non-tumorigenic breast epithelial cell line (MCF-10A). The results indicated that copper conjugate 2 and its nitrogen adducts 3–5 exert significant growth inhibition of cancer cell lines and apoptosis-induction, compared to parent moxifloxacin (1) without any significant effect on non-tumorigenic MCF-10A cells. Interestingly, compound 5 was found to be very active against multiple cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide