Synthesis, Structural Analysis and Antiproliferative Activity of Nitrogen‐Containing Hetero Spirostan Derivatives: Oximes, Heterocyclic Ring‐Fused and Furostanes

Abstract

AbstractThe present study focuses on the synthesis of spirostan derivatives as potential drug candidates for biological applications. Recently, spirostan derivatives containing the hetero‐atom have attracted great scientific attention due to their anti‐cancer, anti‐diabetes, and anti‐inflammatory properties. In this study, nitrogen‐containing novel spirostan derivatives with substituted oxime, nitrile, pyrazole, isoxazole structures in ring‐A and F were designed and synthesized starting from diosgenin. The intermediates and target derivatives’ chemical structures were characterized by FTIR, HRMS, 1HNMR, 13CNMR, elemental analysis, and HPLC techniques. The target compounds were evaluated for their cytotoxicities in two human cancer cell lines (MCF‐7 and A549). The tested compounds exhibited potent anticancer activity against human breast adenocarcinoma (MCF‐7) and lung adenocarcinoma (A549). On the other hand, the toxicity of the tested compounds against human healthy fetal lung fibroblasts (MCR‐5) indicated that compounds were non‐toxic for the human body. The results showed that compounds may be used as a promising agents for anticancer agents with improved efficacy.