| 16-亚甲基雌酮衍生物的合成和抗辐射损伤研究 |
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| 引用本文： | 童曾寿,甘贵之. 16-亚甲基雌酮衍生物的合成和抗辐射损伤研究[J]. 军事医学科学院院刊, 1988, 0(3) |
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| 作者姓名： | 童曾寿 甘贵之 |
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| 作者单位： | 军事医学科学院放射医学研究所，军事医学科学院放射医学研究所 |
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| 摘 要： | 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.
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| 关 键 词： | 辐射防护剂 甾体雌激素 16-亚甲基雌酮衍生物 |
SYNTHESIS AND RADIOPROTECTIVE ACTIVITY OF 16-METHYLENE ESTRONE DERIVATIVES |
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| Tong Zengshou,Gan Guizhi Institute of Radiation Medicine,Academy of Military Medical Sciences. SYNTHESIS AND RADIOPROTECTIVE ACTIVITY OF 16-METHYLENE ESTRONE DERIVATIVES[J]. Bulletin of the Academy of Military Medical Sciences, 1988, 0(3) |
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| Authors: | Tong Zengshou Gan Guizhi Institute of Radiation Medicine Academy of Military Medical Sciences |
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| Abstract: | Eleven compounds were synthesized for evaluation of estrogenic activity and radioprotective effect.It was shown in preliminary tests that introduction of conjugated system into D ring generally resulted in a reduction of the estrogenic activity.Among these compounds,16-hydroxymethylene estrones (1a and 1b) were found to exhibit better protective effect in irradiated mice than estradiol and estriol,whereas 1c-f had no protective activity.2a,2b,4 and 5 showed moderate effect.The structure-activity relationship of 16-methylene estrone derivatives is described. |
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| Keywords: | radioprotector estrogenic steroid 16-methylene estrone derivative |
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