雌酚酮3-醚衍生物的合成与生理活性初探

SYNTHESIS OF ESTRONE 3-ETHERS DERIVATIVES AND PILOT STUDY OF BIOLOGICAL ACTIVITY

目的 合成雌激素 3-醚化合物以观察雌激素活性。方法 以雌酚酮为原料 ,在 3位与碱性侧链相连 ,合成了 4个化合物 ,其中 2个未见文献报道 ,并进行亲子宫和抗子宫活性测定。结果 经初步生理活性测定其雌激素活性明显小于母体化合物。结论 雌激素

OBJECTIVE To synthesize estrogenic compounds with 3-ethers structure to observe estrogenic activities. METHODS Combining estrone with basic side chain on 3-position, four compounds were synthesized, two of them have not been reported, and the activities of compounds were measured by their affinity to uterus. RESULTS Their estrogenic activities appeared obviously lower than that of the matrix compounds. CONCLUSION The estrogenic activities of estrone substituted on 3-position by basic side chains may be changed.