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1
Evaluation of new estrogen-linked 2-chloroethylnitrosoureas. I. Short term anticancer efficacy in methylnitrosourea-induced rat mammary carcinoma and hormonal activity in mice.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
J Cancer Res Clin Oncol. 1984;108(1):148-53. doi: 10.1007/BF00390987.
2
Estrogen-linked 2-chloroethylnitrosoureas: anticancer efficacy in MNU-induced rat mammary carcinoma, uterine activity in mice and receptor interactions.雌激素连接的2-氯乙基亚硝脲：对N-甲基-N-亚硝基脲诱导的大鼠乳腺癌的抗癌疗效、对小鼠子宫的作用及受体相互作用
Eur J Cancer Clin Oncol. 1986 Oct;22(10):1179-91. doi: 10.1016/0277-5379(86)90319-6.
3
Androgen-linked alkylating agents: biological activity in methylnitrosourea-induced rat mammary carcinoma.雄激素相关烷化剂：在甲基亚硝基脲诱导的大鼠乳腺癌中的生物活性
J Cancer Res Clin Oncol. 1990;116(6):538-49. doi: 10.1007/BF01637072.
4
In vitro evaluation of an estradiol-linked nitrosourea in mammary carcinomas of mouse, rat and man.雌二醇连接亚硝基脲在小鼠、大鼠和人类乳腺癌中的体外评估。
Eur J Cancer Clin Oncol. 1988 Jun;24(6):1027-32. doi: 10.1016/0277-5379(88)90153-8.
5
Antineoplastic efficacy of melphalan and N-(2-chloroethyl)-N-nitrosocarbamoyl-omega-lysine, in combination with diazoxide or insulin in autochthonous mammary carcinoma of the Sprague-Dawley rat.美法仑和N-(2-氯乙基)-N-亚硝基氨基甲酰-ω-赖氨酸与二氮嗪或胰岛素联合应用于斯普拉格-道利大鼠自发性乳腺癌的抗肿瘤疗效。
J Cancer Res Clin Oncol. 1990;116(1):45-50. doi: 10.1007/BF01612639.
6
Cytostatic activity of steroid linked nitrosoureas.甾体连接亚硝基脲的细胞生长抑制活性。
J Cancer Res Clin Oncol. 1984;108(1):164-8. doi: 10.1007/BF00390991.
7
Comparison of in vivo and in vitro activity of estrogen-linked nitrosoureas in methylnitrosourea-induced rat mammary carcinoma.雌激素连接亚硝基脲在甲基亚硝基脲诱导的大鼠乳腺癌中的体内和体外活性比较。
J Cancer Res Clin Oncol. 1988;114(3):317-20. doi: 10.1007/BF00405842.
8
Hexadecylphosphocholine differs from conventional cytostatic agents.十六烷基磷胆碱不同于传统的细胞抑制剂。
J Cancer Res Clin Oncol. 1993;119(9):541-8. doi: 10.1007/BF01686464.
9
Evaluation of spin labeled TEPA and CCNU analogs against osteosarcoma and MNU-induced mammary carcinoma of the SD-rat.自旋标记的三乙烯四胺（TEPA）和环己亚硝脲（CCNU）类似物对SD大鼠骨肉瘤和N-甲基-N-亚硝基脲（MNU）诱导的乳腺癌的评估。
Arch Geschwulstforsch. 1989;59(4):251-6.
10
Anticancer efficacy of 2-chloroethylnitrosocarbamoyl derivatives of L-alanine, glycine, their di- and tripeptide homologues and the respective amides in methylnitrosourea-induced rat mammary carcinoma.L-丙氨酸、甘氨酸的2-氯乙基亚硝基甲酰基衍生物、其二肽和三肽同系物以及相应酰胺在甲基亚硝基脲诱导的大鼠乳腺癌中的抗癌疗效
Br J Cancer. 1989 Mar;59(3):335-40. doi: 10.1038/bjc.1989.66.

引用本文的文献

1
Therapeutic ratio of mono or combination bacterial lipopolysaccharide therapy in methylnitrosourea-induced rat mammary carcinoma.单种或联合细菌脂多糖疗法对甲基亚硝基脲诱导的大鼠乳腺癌的治疗比率
J Cancer Res Clin Oncol. 1987;113(5):437-45. doi: 10.1007/BF00390037.
2
Cytotoxic esters of 1,1-bis-(4-hydroxyphenyl)-2-phenyl-but-1-ene with selective antitumor activity against estrogen receptor-containing mammary tumors.1,1-双-（4-羟基苯基）-2-苯基-1-丁烯的具有对含雌激素受体的乳腺肿瘤选择性抗肿瘤活性的细胞毒性酯类
J Cancer Res Clin Oncol. 1987;113(3):230-4. doi: 10.1007/BF00396378.
3
Anti-tumour, toxicological and pharmacokinetic properties of a novel taurine-based nitrosourea (TCNU).一种新型牛磺酸基亚硝基脲（TCNU）的抗肿瘤、毒理学及药代动力学特性
Invest New Drugs. 1988 Apr;6(1):19-30. doi: 10.1007/BF00170775.
4
Comparison of in vivo and in vitro activity of estrogen-linked nitrosoureas in methylnitrosourea-induced rat mammary carcinoma.雌激素连接亚硝基脲在甲基亚硝基脲诱导的大鼠乳腺癌中的体内和体外活性比较。
J Cancer Res Clin Oncol. 1988;114(3):317-20. doi: 10.1007/BF00405842.
5
Modulation of cytosolic sexual steroid receptors in autochthonous methylnitrosourea-induced rat mammary carcinoma following application of 2-chloroethylnitrosocarbamoyl-L-alanine linked to oestradiol or dihydrotestosterone.在应用与雌二醇或二氢睾酮相连的2-氯乙基亚硝基氨基甲酰-L-丙氨酸后，对原位甲基亚硝基脲诱导的大鼠乳腺癌中细胞溶质性激素受体的调节。
Br J Cancer. 1990 Jul;62(1):42-7. doi: 10.1038/bjc.1990.226.
6
The pharmacokinetic model and distribution pattern of new sexual-steroid-hormone-linked anticancer agents.新型性甾体激素连接抗癌药物的药代动力学模型及分布模式。
J Cancer Res Clin Oncol. 1990;116(5):467-9. doi: 10.1007/BF01612995.

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[Specific chemotherapy of carcinoma of the prostate].[前列腺癌的特异性化疗]
Klin Wochenschr. 1952 Oct 1;30(37-38):882-4. doi: 10.1007/BF01471475.
2
[Development of new antiestrogens of the 3,3'-dihydroxy-alpha, beta-diethylstilbene-type and their evaluation on the DMBA-induced hormone dependent mammary carcinoma of the SD-rat (author's transl)].[3,3'-二羟基-α,β-二乙基芪型新型抗雌激素的研制及其对二甲基苯并蒽诱导的SD大鼠激素依赖性乳腺癌的评价（作者译）]
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Examination of newly synthesized 2-chloroethyl-nitrosoureas on rat leukemia L 5222.新型合成的2-氯乙基亚硝基脲对大鼠白血病L 5222的研究。
Oncology. 1981;38(1):39-42. doi: 10.1159/000225519.
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Drug interaction with estrogen receptors for the control of breast neoplasia (review).用于控制乳腺肿瘤的雌激素受体药物相互作用（综述）
Anticancer Res. 1981;1(4):217-28.
5
Noncarcinogenic chemotherapy with a combination of vincristine, methotrexate and 5-fluorouracil (VMF) in rats.在大鼠中使用长春新碱、甲氨蝶呤和5-氟尿嘧啶（VMF）联合进行非致癌性化疗。
Int J Cancer. 1983 Aug 15;32(2):231-6. doi: 10.1002/ijc.2910320215.
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Examination of newly synthesized 2-chloroethylnitrosoureas in preterminal leukemia L 5222 and in two transplanted neurogenic tumors.
Arzneimittelforschung. 1982;32(5):481-4.
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Studies on the mechanism of action of LS 1727, a nitrosocarbamate of 19-nortestosterone.关于19-去甲睾酮亚硝基氨基甲酸酯LS 1727作用机制的研究。
Acta Pharmacol Toxicol (Copenh). 1981 Feb;48(2):129-38. doi: 10.1111/j.1600-0773.1981.tb01598.x.
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Synthesis of steroidal cyclophosphamides.甾体环磷酰胺的合成。
Steroids. 1976 Mar;27(3):353-60. doi: 10.1016/0039-128x(76)90056-8.
9
Some new congeners of the anticancer agent 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU). Synthesis of bifunctional analogs and water soluble derivatives and preliminary evaluation of their chemotherapeutic potential.抗癌剂1,3-双（2-氯乙基）-1-亚硝基脲（卡莫司汀）的一些新同系物。双功能类似物和水溶性衍生物的合成及其化疗潜力的初步评估。
Z Krebsforsch Klin Onkol Cancer Res Clin Oncol. 1976 Aug 30;86(3):279-86. doi: 10.1007/BF00286946.
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Synthesis of steroidal nitrosoureas with antitumor activity.具有抗肿瘤活性的甾体亚硝基脲的合成。
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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.

DOI:10.1007/BF00390987
PMID:6746705
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12252557/
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。