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- W1984309968 abstract "Abstract The enzyme aromatase, responsible for the production of the estrogen hormones in human females is currently a priority target for the development of active-site directed inhibitors which may have potential for the control of estrogen-dependent diseases e.g. breast cancer. As part of a continuing study aimed at probing the aromatase active site through the use of steroidal inhibitors, we have synthesized the novel 6,7-aziridinyl steroids and other related compounds (fused steroidal oxiranes, azides and azidohydrins). The stereospecific synthesis of the 6α,7α and 6β,7β-aziridines was accomplished by treatment of an appropriate vicinal azidohydrin with triphenylphosphine. These compounds were evaluated as inhibitors of human placental aromatase. Most of the compounds were modest inhibitors of the enzyme (IC50 values 3.03 μM – 49.25 μM). The inhibitory behaviour of the 6,7-aziridinyl steroids will be discussed and compared with that of 6,7-cyclopropane derivatives of androst-4-ene-17-ones which are potent inhibitors of human placental aromatase." @default.
- W1984309968 created "2016-06-24" @default.
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- W1984309968 date "1994-09-01" @default.
- W1984309968 modified "2023-09-23" @default.
- W1984309968 title "FC25 synthesis and evaluation of 6α,7α- and 6β,7β-aziridinylandrost-4-ENE-3,17-diones and related compounds as potential aromatase inhibitors" @default.
- W1984309968 doi "https://doi.org/10.1016/0928-0987(94)90134-1" @default.
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