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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Synthesis and anti-aromatase activity of some new steroidal D-lactones.

Starting from D-seco derivatives of 5-androstene 1-3, the D-homo lactones, 4 and 5, were synthesized. By the Oppenauer oxidation and/or by dehydration of 4 and 5 with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) or 2,3,5,6-tetrachloro-1,4-benzoquinone (chloranil), the corresponding D-lactones 6-12 were obtained. The structures of 6 and 10 were unambiguously proved by the appropriate X-ray structural analysis. Anti-aromatase assay showed that tested compounds possess inhibition potency, however, two to four times smaller (IC50 from 0.2 to 0.7 microM, respectively) in comparison to aminoglutethimide (AG).[1]

References

  1. Synthesis and anti-aromatase activity of some new steroidal D-lactones. Gasi, K.M., Stojanović, S.Z., Sakac, M.N., Popsavin, M., Santa, S.J., Stanković, S.M., Klisurić, O.R., Andrić, N., Kovacević, R. Steroids (2005) [Pubmed]
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