Semi-synthesis and biological activities of heterocyclic compounds containing camphor

Abstract

Breast cancer and lung cancer are two of the most prevalent and deadly malignancies worldwide. Both cancers present significant challenges in terms of effective treatment and management, highlighting the urgent need for novel therapeutic strategies that can improve patient outcomes. This study focuses on the synthesis of novel heterocyclic compounds derived from the naturally formed camphor, aimed at evaluating their cytotoxicity. The research addresses the need for effective cancer treatments by presenting compounds that demonstrate significant inhibitory effects against MCF-7 breast carcinoma cells. Among these, compound 20 exhibited remarkable potency, with an IC₅₀ value of 0.78 μM, surpassing the efficacy of standard chemotherapeutics, dasatinib (IC₅₀ = 7.99 μM) and doxorubicin (IC₅₀ = 3.10 μM). In the context of A549 lung cancer cells, compound 20 also showed strong inhibitory activity (IC₅₀ = 1.69 μM), again outperforming dasatinib (IC₅₀ = 11.8 μM) and doxorubicin (IC₅₀ = 2.43 μM). To further elucidate the biological activities of these compounds, molecular docking studies were performed, revealing that compound 20 exhibited the highest binding energy among the tested compounds, supporting the experimental findings. These results indicate that the synthesized camphor-derived heterocycles, particularly compound 20, have significant potential as potent anticancer agents against breast and lung cancer cell lines.