新型雌激素连接的2-氯乙基亚硝脲的评估。I. 对甲基亚硝脲诱导的大鼠乳腺癌的短期抗癌疗效及对小鼠的激素活性
Evaluation of new estrogen-linked 2-chloroethylnitrosoureas. I. Short term anticancer efficacy in methylnitrosourea-induced rat mammary carcinoma and hormonal activity in mice.
作者信息
Berger M R, Floride J, Schreiber J, Schmähl D, Eisenbrand G
出版信息
J Cancer Res Clin Oncol. 1984;108(1):148-53. doi: 10.1007/BF00390987.
Abstract
Short-term treatment of N-methyl-N-nitrosourea-induced mammary carcinomas in Sprague-Dawley rats with estradiol-linked nitrosoureas shows that the compounds in which the cytotoxic group is linked to position 17 of estradiol are superior to the 3-ester analogue. Moreover, N-(2-chloroethyl)-N-nitroso-carbamoyl (CNC)-L-alanyl-L-alanine-estradiol-3-ester is more effective and less toxic than CNC-L-alanine-estradiol-3-ester, being equivalent to ovariectomy in its therapeutic efficacy. Unlinked CNC-amino acid or-dipeptide in admixture with estradiol is less effective. Linked compounds at therapeutic dosages display estrogenic activity.
摘要
用与雌二醇相连的亚硝基脲对斯普拉格-道利大鼠的N-甲基-N-亚硝基脲诱导的乳腺癌进行短期治疗，结果表明，细胞毒性基团与雌二醇17位相连的化合物优于3-酯类似物。此外，N-(2-氯乙基)-N-亚硝基氨基甲酰基(CNC)-L-丙氨酰-L-丙氨酸-雌二醇-3-酯比CNC-L-丙氨酸-雌二醇-3-酯更有效且毒性更小，其治疗效果与卵巢切除术相当。未相连的CNC-氨基酸或二肽与雌二醇混合使用效果较差。治疗剂量的相连化合物具有雌激素活性。
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