Phenyliiole derivative 8. linked to aziridine by a hexamethylene spacer group, was synthesized and tested. It binds to the estrogen receptor with an MA-value of 4.0 (estradiol = 100). In v i m , it shows a selective cytostatic activity in hormone-dependent MCF-7 breast cancer cells (41% T/C at 10' M
Labeled steroids of potential biological interest: Synthesis and properties of 180-labeled 17 α-hydroperoxypro-gesterone
✍ Scribed by Pierre Falardeau; Liat Tan
- Publisher
- John Wiley and Sons
- Year
- 1974
- Tongue
- French
- Weight
- 355 KB
- Volume
- 10
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
Abstract
^18^Oxygen labeled 17α‐hydroperoxyprogesterone has been synthesized via a 3‐step reaction sequence in an all‐glass, high vacuum transfer system. The hydroperoxidation reaction was found to proceed smoothly only, when an adequate oxygen pressure in the reaction vessel is maintained. Comparisons are made between the mass spectral fragmentations of the ordinary ^16^O, and the isotopically labeled ^18^0–17α‐hydroperoxyprogesterones. Their NMR‐spectra display a splitting of the 18‐, and 31‐methyl signals, probably due to the coexistence of two finite conformations of the acetyl side‐chain.
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