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设计合成了以籍次乙基为桥将雌激素通过 3 OH醚化与 4种不同哌嗪环相连的衍生物 ,包括中间体共合成了 12个化合物 ,其中 8个目标物及 3个中间体未见文献报道 .结构经质谱、核磁共振谱、红外光谱及元素分析确定 .同时测定了目标物对体外培养小鼠胚胎长骨生长的影响 ,结果显示由雌酚酮和雌二醇与不同的哌嗪环相连所得到的衍生物抑制骨吸收、促进骨形成的作用均不低于相应的母体雌激素 .表明哌嗪环的引入不影响雌激素对骨的药理作用 ,所合成的 4种化合物可以作为骨靶向雌激素的弹头 ,进一步与骨靶向载体连接 .
Design and synthesis of derivatives of ethylenically ethylated estrogens linked to 4 different piperazine rings by ethylethylidene bridged, including 12 intermediates, 12 of which were synthesized and 8 of them were targeted and 3 intermediates The results of mass spectrometry, nuclear magnetic resonance spectroscopy, infrared spectroscopy and elemental analysis determined the effect of the target substance on the growth of long bones of mouse embryos cultured in vitro, and the results showed that the effects of estrone and estradiol The results showed that the introduction of piperazine ring did not affect the pharmacological effects of estrogen on bone, and the four compounds synthesized could be As a bone-targeted estrogen bullet, it is further linked to a bone-targeting vector.