Bioactivity studies of two copper complexes based on pyridinedicarboxylic acid N-oxide and 2,2′-bipyridine

Bioactivity of two heteroleptic copper complexes based on pyridinedicarboxylic acid N-oxide and 2,2'bipyridine which benefit from extensive hydrogen bonds and pi-interactions is reported. Anti-cancer activities of 1 and 2 were evaluated by MTT assay against a panel of murine and human cancer cell lines. Moreover, the synergistic effects of 1 in combination with cisplatin, paclitaxel, and topotecan were investigated on HeLa cells. Cell death mechanism induced by 1 was also assessed using FITC-annexin V/PI staining. MTT results indicated that 1 inhibited the proliferation of cancerous cells as compared with normal cells. Complex 2 also exerted selective toxicity towards both murine and human colon cancer cells. Moreover, the strongest synergistic effect was obtained from the combination of 1 with topotecan, and apoptosis was the main mechanism of cell death. Our results indicated that both complexes significantly inhibited the proliferation of cancerous cells. Furthermore, complex 1 can be a promising chemotherapeutic agent to be used in combination with other drugs for treatment of cervical cancer, although more studies are required to confirm this. (C) 2021 Elsevier B.V. All rights reserved.

Automated summary

The bioactivity of two heteroleptic copper complexes based on pyridinedicarboxylic acid N-oxide and 2,2'bipyridine with potential anti-cancer activities was reported. Complex 1 exhibited the strongest synergistic effect when combined with topotecan, with apoptosis being the main mechanism of cell death. Overall, the complexes significantly inhibited the proliferation of cancerous cells and complex 1 showed promise as a potential chemotherapeutic agent for cervical cancer treatment when used in combination with other drugs.