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环磷酰胺和异环磷酰胺的 /+/R 及 /-/S 对映体生物活性的比较研究。I. 环磷酰胺和异环磷酰胺对映体的抗肿瘤作用。

Comparative studies on biological activity of /+/R and /-/S enantiomers of cyclophosphamide and ifosfamide. I. Antitumour effect of cyclophosphamide and ifosfamide enantiomers.

作者信息

Paprocka M, Kuśnierczyk H, Budzyński W, Rak J, Radzikowski C

出版信息

Arch Immunol Ther Exp (Warsz). 1986;34(3):275-84.

PMID:3592931
Abstract

The differences in antitumour effect of /+/R and /-/S enantiomers of both cyclophosphamide and ifosfamide were detected. In the case of ifosfamide in all five tested tumour models (Leukemia L1210, P388, Lewis lung carcinoma, 16/C mammary adenocarcinoma and B16 melanoma) the /-/S form exerted not only higher antitumour effects than /+/R form, but revealed higher therapeutic indices as well. The same appeared to be true for /-/S enantiomer of cyclophosphamide in three models of solid tumours. In L1210 and P-388 ascitic leukemia models /+/R and /-/S cyclophosphamide exerted the same antitumour effect.

摘要

检测了环磷酰胺和异环磷酰胺的 /+/R 和 /-/S 对映体在抗肿瘤效果上的差异。就异环磷酰胺而言,在所有五个测试的肿瘤模型(白血病 L1210、P388、Lewis 肺癌、16/C 乳腺腺癌和 B16 黑色素瘤)中,/-/S 形式不仅比 /+/R 形式具有更高的抗肿瘤效果,而且还显示出更高的治疗指数。环磷酰胺的 /-/S 对映体在三种实体瘤模型中似乎也是如此。在 L1210 和 P - 388 腹水白血病模型中,/+ /R 和 /-/S 环磷酰胺具有相同的抗肿瘤效果。

相似文献

1
Comparative studies on biological activity of /+/R and /-/S enantiomers of cyclophosphamide and ifosfamide. I. Antitumour effect of cyclophosphamide and ifosfamide enantiomers.环磷酰胺和异环磷酰胺的 /+/R 及 /-/S 对映体生物活性的比较研究。I. 环磷酰胺和异环磷酰胺对映体的抗肿瘤作用。
Arch Immunol Ther Exp (Warsz). 1986;34(3):275-84.
2
Comparative studies on biological activity of /+/R and /-/S enantiomers of cyclophosphamide and ifosfamide. II. Antiproliferative activity of cyclophosphamide and ifosfamide enantiomers.环磷酰胺和异环磷酰胺的 /+/R 及 /-/S 对映体的生物活性比较研究。II. 环磷酰胺和异环磷酰胺对映体的抗增殖活性。
Arch Immunol Ther Exp (Warsz). 1986;34(3):285-91.
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Isophosphoramide mustard, a metabolite of ifosfamide with activity against murine tumours comparable to cyclophosphamide.异环磷酰胺氮芥,异环磷酰胺的一种代谢产物,其对鼠肿瘤的活性与环磷酰胺相当。
Br J Cancer. 1983 Jan;47(1):15-26. doi: 10.1038/bjc.1983.2.
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1
Pharmacokinetics of ifosfamide and its enantiomers following a single 1 h intravenous infusion of the racemate in patients with small cell lung carcinoma.在小细胞肺癌患者中单次静脉输注消旋体1小时后异环磷酰胺及其对映体的药代动力学。
Br J Clin Pharmacol. 1995 Apr;39(4):452-5. doi: 10.1111/j.1365-2125.1995.tb04477.x.