Synthesis, NMR characterization and cytotoxic activity of hybrid spirostanic sapogenins-estradiol dimers.

Four hybrid steroid dimers were obtained by BF ₃ ·Et ₂ O-catalyzed aldol condensation of acetylated steroid sapogenins with 2-formyl-estradiol diacetate. The structures of the obtained dimers were unambiguously established by NMR. The hybrid dimers 9a (IC ₅₀ 18.37 μM) and 9c (IC ₅₀ 9.4 μM) with the 5α configuration at the A/B rings junction showed the higher cytotoxicity against HeLa, with selectivity index of 4.36 and 11.8 respectively. The presence of a carbonyl function at position C-12 produced the highest cytotoxic effect, which is in line with our previous reports.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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