Sonnet P, Guillon J, Enguehard C, Dallemagne P, Bureau R, Rault S Auvray P, Moslemi S, Sourdiane P, Galopin S, Séralini G E
Centre d'Etudes et de Recherche sur le Médicament de Normandie, Laboratoire de Pharmacochimie, Caen, France.
Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4. doi: 10.1016/s0960-894x(98)00157-7.
The structure-activity relationship study of one of recently described aromatase inhibitors, compound 1 (MR20814), allowed us to design some related derivatives as potential new inhibitors. Among those we synthesized, chlorophenylpyridylmethylenetetrahydroindolizinone 5 (MR20492) exhibited in vitro a ten-fold higher inhibition of the enzyme (IC50 = 0.2 +/- 0.0 microM and Ki = 10.3 +/- 3.3 nM).
对最近报道的一种芳香酶抑制剂化合物1（MR20814）的构效关系研究，使我们能够设计一些相关衍生物作为潜在的新型抑制剂。在我们合成的这些衍生物中，氯苯基吡啶基亚甲基四氢吲哚嗪酮5（MR20492）在体外对该酶的抑制作用高十倍（IC50 = 0.2 +/- 0.0微摩尔，Ki = 10.3 +/- 3.3纳摩尔）。
