倪元, 郝日英, 周维善. 7α和7β-甲基-10β,17β-二乙酰氧基-4-雌甾烯-3-酮的合成J. 药学学报, 1987, 22(7): 495-500.
引用本文: 倪元, 郝日英, 周维善. 7α和7β-甲基-10β,17β-二乙酰氧基-4-雌甾烯-3-酮的合成J. 药学学报, 1987, 22(7): 495-500.
NI Yuan, HAO Ri-Ying , ZHOU Wei-Shan, . SYNTHESIS OF 7α-METHYL AND 7β-METHYL-10β,17β-DIACETOXY-4-ESTRENE-3-ONEJ. Acta Pharmaceutica Sinica, 1987, 22(7): 495-500.
Citation: NI Yuan, HAO Ri-Ying , ZHOU Wei-Shan, . SYNTHESIS OF 7α-METHYL AND 7β-METHYL-10β,17β-DIACETOXY-4-ESTRENE-3-ONEJ. Acta Pharmaceutica Sinica, 1987, 22(7): 495-500.

7α和7β-甲基-10β,17β-二乙酰氧基-4-雌甾烯-3-酮的合成

SYNTHESIS OF 7α-METHYL AND 7β-METHYL-10β,17β-DIACETOXY-4-ESTRENE-3-ONE

  • 摘要: 由于7α-甲基或10β-乙酰氧基4(5)烯-3-酮雌(雄)甾化合物具有显著的抗着床或抗蜕膜活性,我们合成了既具有7α-甲基或7β-甲基又具有10β-乙酰氧基的两个新甾族化合物(1a)和(1b)。经药理试验表明(1a)和(1b)对孕鼠均有抗早孕作用。

     

    Abstract: Since 7α-methyl or 10β-acetoxyestrene-3-ketones were known to show significant anti-implantational or anti-decidual activities, we have synthesized two new steroidal ketones (1a). and (1b) possessing both the 7α-or 7β-methyl group and the 10β-acetoxy substitutions according to scheme 1.Experimental animal tests of (1a) showed that it was effective for termination of early pregnancy on mice with the success rate of 100% (4mg/kg). (1a) is approximately 3~4 times more potent than (1b). Results of parmacological tests have been reported elsewhere.

     

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