Design and synthesis of novel triazolo-lapatinib hybrids as inhibitors of breast cancer cells

AbstractA series of triazolo-lapatinib hybrids were synthesized via copper (II)-oxide nanoparticle (Cu2O-NP)-catalyzed azide-alkyne cycloaddition. The ability of these compounds to reduce the viability of breast cancer SKBR3 and SUM159 cells and stem cell-like KG-1a leukemia cells was subsequently evaluated. Compared with lapatinib, compounds6c–f were more potent than lapatinib against the three cell lines. Next, the toxicity of compounds6c–f was assessed in zebrafish. Compound6d had comparable toxicity with lapatinib at 200  μM (mortality rate = 10 vs. 10%), and compound6e had lower toxicity than lapatinib at 200  μM (mortality rate = 0 vs. 10%). Thus, compound6e is a promising lead compound worthy of further investigation.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research