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本文比较了炔诺酮肟(NETO)、炔诺酮(NET)、醋炔诺酮肟(NETO-Ac)、醋炔诺酮(NET-Ac)、18-甲基炔诺酮肟(NGTO)、18-甲基炔诺酮(NGT)、醋18-甲基炔诺酮肟(NGTO-Ac)和醋18-甲基炔诺酮(NGT-Ac)8种化合物的雌激素活性及对兔子宫胞浆雌二醇(E_2)受体的亲和力。实验结果证实:NETO的雌激素活性及对E_2受体的亲和力比母体NET明显增强。NETO-Ac及NGTO-Ac也比相应的母体化合物NET-Ac及NGT-Ac有所增强,表明C_3位酮基肟化后,雌激素活性及对受体的亲和力都有增强的趋势。而炔诺酮类C_(18)甲基化后,雌激素活性及对雌二醇受体的亲和力均比相应的母体化合物有所下降。
This article compared NETO, NET, NETO-Ac, NET-Ac, 18-norethindrone oxime (NGTO) , Estrogen activity of 8 compounds including 18-norgestrel (NGT), vinegar 18-norgestrel oxime (NGTO-Ac) and vinegar 18-norgestrel Uterine cytoplasmic estradiol (E2) receptor affinity. Experimental results show that: NETO estrogen activity and E_2 receptor affinity than the mother NET was significantly enhanced. NETO-Ac and NGTO-Ac also increased compared with the corresponding parent compounds NET-Ac and NGT-Ac, indicating that the estrogen activity and receptor affinity of C_3 ketoxitine increased. However, the methylation of norethindrone C_ (18) decreased estrogen activity and estradiol receptor affinity than the corresponding parent compounds.