von Angerer E, Prekajac J, Schneider M R, Berger M R
J Cancer Res Clin Oncol. 1985;110(3):216-20. doi: 10.1007/BF00399276.
The antineoplastic activity of 4-chloro-2-(2,6-dichloro-4-hydroxyphenyl)-1-ethyl-6-hydroxyindole (D 15413) was determined in several estrogen-dependent mammary tumor models. The growth of DMBA-induced rat mammary carcinomas was inhibited by doses ranging from 2 to 18 mg/kg. A dose of 6 X 12 mg/kg per week p.o. reduced the tumor area by 82% (control + 192%). D 15413 was also active against MNU-induced rat mammary tumors and transplanted MXT tumors of the mouse. In vitro, the growth of estrogen receptor positive MCF-7 breast cancer cells was inhibited by D 15413 (10(-8) - 10(-5) M). A mode of action considering endocrine and cytotoxic effects is discussed.
在几种雌激素依赖性乳腺肿瘤模型中测定了4-氯-2-(2,6-二氯-4-羟基苯基)-1-乙基-6-羟基吲哚（D 15413）的抗肿瘤活性。二甲基苯并蒽（DMBA）诱导的大鼠乳腺癌生长受到2至18mg/kg剂量的抑制。每周口服6×12mg/kg的剂量可使肿瘤面积减少82%（对照组为+192%）。D 15413对N-甲基-N-亚硝基脲（MNU）诱导的大鼠乳腺肿瘤和小鼠移植的MXT肿瘤也有活性。在体外，D 15413（10⁻⁸ - 10⁻⁵M）可抑制雌激素受体阳性的MCF-7乳腺癌细胞的生长。讨论了一种考虑内分泌和细胞毒性作用的作用模式。
