von Angerer E, Prekajac J, Berger M
Eur J Cancer Clin Oncol. 1985 Apr;21(4):531-7. doi: 10.1016/0277-5379(85)90048-3.
The antineoplastic activity of the antiestrogen 5-acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole (D 16726) was determined in several estrogen-dependent mammary tumor models. The growth of the DMBA-induced rat mammary carcinoma was inhibited by doses ranging from 1 to 12 mg/kg. The maximum decrease of tumor area was 67% (control + 635%). D 16726 was also active against MNU-induced rat mammary tumors and transplanted MXT tumors of the mouse. The growth of estrogen receptor-positive MCF-7 breast cancer cells was inhibited by the hydroxy derivative D 15414 (10(-8)-10(-5) M). Because of the high binding affinity of D 15414 for the estrogen receptor (RBA 6.7-10.0) and the lack of activity against hormone-independent MDA-MB 231 breast cancer cells, a specific mode of action involving the estrogen receptor is likely.
在几种雌激素依赖性乳腺肿瘤模型中评估了抗雌激素5-乙酰氧基-2-（4-乙酰氧基苯基）-1-乙基-3-甲基吲哚（D 16726）的抗肿瘤活性。DMBA诱导的大鼠乳腺癌的生长受到1至12 mg/kg剂量的抑制。肿瘤面积的最大减少量为67%（对照组为+635%）。D 16726对MNU诱导的大鼠乳腺肿瘤和小鼠移植的MXT肿瘤也有活性。雌激素受体阳性的MCF-7乳腺癌细胞的生长受到羟基衍生物D 15414（10^-8 - 10^-5 M）的抑制。由于D 15414对雌激素受体具有高结合亲和力（相对结合亲和力为6.7 - 10.0）且对激素非依赖性的MDA-MB 231乳腺癌细胞无活性，因此可能存在涉及雌激素受体的特定作用模式。
