Taylor H M, Jones C D, Davenport J D, Hirsch K S, Kress T J, Weaver D
J Med Chem. 1987 Aug;30(8):1359-65. doi: 10.1021/jm00391a016.
The inhibition of estrogen biosynthesis has been suggested to be an effective treatment of hormone-dependent diseases, particularly breast cancer. Several series of 5-substituted pyrimidine derivatives have been synthesized and tested for their ability to inhibit the enzyme aromatase (estrogen synthetase). Compounds were evaluated in an in vitro assay that measured the inhibition of rat ovarian microsomal aromatase activity. Greatest inhibitory activity was achieved in the cases of diarylpyrimidinemethanols and diarylpyrimidinyl methanes which were substituted in the 4- and 4'-positions with electron-withdrawing substituents, particularly Cl.
抑制雌激素生物合成已被认为是治疗激素依赖性疾病，尤其是乳腺癌的有效方法。已经合成了几系列5-取代嘧啶衍生物，并测试了它们抑制芳香化酶（雌激素合成酶）的能力。在一项体外试验中对化合物进行评估，该试验测量大鼠卵巢微粒体芳香化酶活性的抑制情况。在4-位和4'-位被吸电子取代基（尤其是Cl）取代的二芳基嘧啶甲醇和二芳基嘧啶甲烷的情况下，实现了最大抑制活性。
