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人乳腺癌中富含雌激素受体,因此发展浓集于乳腺癌的γ-放射性雌激素作为癌显象剂的工作引起了重视。这种特异性显象剂在体内给药后,可无损地提供原发性和转移性乳腺癌的诊断资料。作者合成了一系列己烷雌酚和雌二醇的卤代衍生物,并以雌二醇为标准(受体结合力规定为100%),用竞争性结合分析法,测量化合物对子宫雌激素受体的相对结合力。结果发现:(1)芳卤代己烷雌酚中,邻-氟乙烷雌酚(A)的结合力最高(205%),但相应的溴、碘衍生物的结合力都极低(<16%);(2)侧链卤代己烷雌酚衍生物中,氟代己烷雌酚与受体结合力最高(129%),氯
Human breast cancer is rich in estrogen receptors, so the development of breast cancer-concentrated γ-radioactive estrogen as a carcinogen imaging work has drawn great attention. This specific imaging agent provides diagnostic information on primary and metastatic breast cancer nondestructively after in vivo administration. The authors synthesized a series of halogenated derivatives of diethylstilbestrol and estradiol and used estradiol as a standard (receptor binding was defined as 100%). The compounds were tested for their effect on uterine estrogen The relative binding of receptors. The results showed that: (1) The highest affinity of o-haloethanethol (A) (205%) was found in the aromatic halohexestroloesters, but the corresponding bromine and iodine derivatives showed very low binding (< 16%); (2) Among the side-chain halogenated hexa-estreso derivatives, hexa-estrone has the highest binding affinity with receptor (129%), chlorine