Arunachalam T, Longcope C, Caspi E
J Biol Chem. 1979 Jul 10;254(13):5900-5.
The rationale for undertaking the present study was to evaluate the utility of iodoestradiol analogs made highly radioactive with iodine isotopes in (a) the non-invasive differentiation of estrogen-dependent from estrogen-independent breast tumors, (b) spread of metastases containing estrogen receptors, and (c) potential application in therapeutic irradiation of target tissues. In the present paper, the model syntheses of a number of nonradioactive 127I-estrogen analogs are described. The analogs were tested for their ability to displace (compete with) [3H]estradiol from receptor sites. The most active compounds, 16beta-iodoestra-1,3,5(10)-triene-3,17 beta-diol (17) and 6-iodoestra-1,3,5(10),6-tetraene-3,17 beta-diol (10b), showed a relative binding affinity of 0.57 and 0.49, respectively.
（a）对雌激素依赖性和非雌激素依赖性乳腺肿瘤进行非侵入性鉴别，（b）含雌激素受体转移灶的扩散，以及（c）在靶组织治疗性放射中的潜在应用。在本文中，描述了多种非放射性127I-雌激素类似物的模型合成。测试了这些类似物从受体位点取代（竞争）[3H]雌二醇的能力。活性最高的化合物，16β-碘-1,3,5(10)-雌三烯-3,17β-二醇（17）和6-碘-1,3,5(10),6-雌四烯-3,17β-二醇（10b），相对结合亲和力分别为0.57和0.49。
