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本文报道合成了11个标题化合物,其中7个为新化合物.其结构用元素分析及波谱分析证明.对化合物的抗辐射损伤及雌活力进行了评定.药理试验初步结果提示,雌甾D环引入双键或带双键的官能团,一般雌活力降低.这些化合物中16-羟亚甲基雌酮(la和lb)对受照小鼠的抗辐射活性(分别减低133及95rad)比E_2及E_3的抗辐射活性高(降低75和55rad)而1c～f则无抗辐射活性.2a,2b,4和5具有中度抗辐射作用.文中还讨论了构效关系.
In this paper, 11 title compounds were synthesized, of which 7 were new compounds.The structure was confirmed by elemental analysis and spectroscopic analysis.The anti-radiation damage and the viability of the compounds were evaluated.The preliminary results of the pharmacological tests suggested that the introduction of the estrogen D ring Double bond or a functional group with a double bond, generally decreased the viability of the mice.The anti-radiation activity of these compounds against irradiated mice (133 and 95 rad, respectively) was lower than that of E 2 and E 3 (75 and 55 rad), while 1c-f showed no anti-radiation activity.2a, 2b, 4 and 5 had moderate anti-radiation effects.The structure-activity relationship was also discussed.