کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5516635 | 1542686 | 2017 | 8 صفحه PDF | دانلود رایگان |
- Synthesis novel chiral heterocycle-fused steroids based on [8ÏÂ +Â 2Ï] cycloadditions.
- Biological evaluation of a new family of hexacyclic steroids as anti-cancer agents.
- Conclusions regarding structure-activity relationships could be withdrawn.
- A benzyl group at C24 is important to ensure cytotoxicity against EL4.
Regio- and stereoselective synthesis of novel chiral 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused steroids via [8ÏÂ +Â 2Ï] cycloaddition of diazafulvenium methides with steroidal scaffolds is reported. The biological evaluation of the new family of hexacyclic steroids as anti-cancer agents was also carried out. Hexacyclic steroids bearing a benzyl group at C-22, derived from 16-dehydropregnenolone and 16-dehydroprogesterone, show considerable cytotoxicity against EL4 (murine T-lymphoma) in contrast with the corresponding C-22-unsubstituted derivatives showing low cytotoxicity. Thus, results indicate that the presence of the benzyl group is important to ensure cytotoxicity.
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Journal: Steroids - Volume 122, June 2017, Pages 16-23