Synthesis and anti-aromatase activity of some new steroidal D-lactones |
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| Authors: | Gasi Katarina M Penov Stojanović Srdjan Z Sakac Marija N Popsavin Mirjana Santa Suzana Jovanović Stanković Slobodanka M Klisurić Olivera R Andrić Nebojsa Kovacević Radmila |
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| Institution: | Department of Chemistry, Faculty of Sciences, University of Novi Sad, 21000 Novi Sad, Trg Dositeja Obradovi?a 3, Serbia and Montenegro, Yugoslavia. sazvon@eunet.yu |
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| Abstract: | 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). |
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| Keywords: | Androgens Steroidal D-lactones Aromatase inhibitors X-ray analysis |
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