氟他莫昔芬类似物的合成及体外受体结合研究
Synthesis and in vitro receptor binding studies of fluorotamoxifen analogues.
作者信息
Yang D J, Wallace S, Tansey W, Wright K C, Kuang L R, Tilbury R S, Diego I, Lim J L, Emran A M, Kim E E
机构信息
Division of Diagnostic Imaging, University of Texas, M. D. Anderson Cancer Center, Houston 77030.
出版信息
Pharm Res. 1991 Feb;8(2):174-7. doi: 10.1023/a:1015879717742.
We describe the synthesis of new fluorotamoxifen analogues with the fluorine atom positioned on the end of the aliphatic chain of tamoxifen. The binding of fluorotamoxifens to cytosol estrogen receptors of rat uteri was determined with [3H]estradiol (5 nM). The fluorotamoxifens had similar or superior binding affinities compared with tamoxifen. The IC50 value was as follows: tamoxifen, 5 x 10(-7) M; fluorotamoxifen (VII), 5 x 10(-7) M; N,N-diethylfluorotamoxifen (IV)-cis, 1 x 10(-6) M, and trans, 2 x 10(-7) M; and (cis) fluoromethyl-N,N-diethyltamoxifen (VI) 1 x 10(-7) M. Therefore, the fluorinated tamoxifens have potential use in imaging estrogen receptors by PET.
我们描述了将氟原子置于他莫昔芬脂肪链末端的新型氟他莫昔芬类似物的合成。用[³H]雌二醇（5 nM）测定氟他莫昔芬与大鼠子宫胞质雌激素受体的结合。与他莫昔芬相比，氟他莫昔芬具有相似或更高的结合亲和力。半数抑制浓度（IC50）值如下：他莫昔芬为5×10⁻⁷ M；氟他莫昔芬（VII）为5×10⁻⁷ M；N,N - 二乙基氟他莫昔芬（IV） - 顺式为1×10⁻⁶ M，反式为2×10⁻⁷ M；以及（顺式）氟甲基 - N,N - 二乙基他莫昔芬（VI）为1×10⁻⁷ M。因此，氟化他莫昔芬在通过正电子发射断层扫描（PET）对雌激素受体进行成像方面具有潜在用途。
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