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[呋瑞齐尔的抗肿瘤活性及药理特性]

[Antitumor activity and pharmacological properties of furizil].

作者信息

Stukov A N, Kraĭz B O, Aleksandrov V A, Ivin B A, Filov V A

出版信息

Vopr Onkol. 1985;31(5):52-4.

PMID:4013130
Abstract

The paper discusses the biological properties of 2-(2-furyl)-5-oxymethyl-5-(2,4-diethyleneimino-1,3,5-triazine- 6-yl) amino-1,3-dioxane (furizil), synthesized by substituting ethyleneimine groups for chlorine atoms in individual stereoisomer of a dichlorotriazine derivative. Furizil was found to inhibit the growth of Ehrlich's tumor, Walker's carcinosarcoma, sarcoma 45 and rat ovarian tumors, the inhibition rate ranging 76-100%. Parenterally administered, LD50 appeared to be 6 mg/kg for rats and 15 mg/kg for mice. Studies of chronic toxicity established damaging effects of furizil on hematopoietic, gastrointestinal and reproductive organs. Toxic effects subsided 1-2 weeks after the drug withdrawal.

摘要

本文讨论了2-(2-呋喃基)-5-氧甲基-5-(2,4-二乙基亚氨基-1,3,5-三嗪-6-基)氨基-1,3-二氧六环(呋立齐)的生物学特性。呋立齐是通过用乙亚胺基团取代二氯三嗪衍生物的单个立体异构体中的氯原子合成的。发现呋立齐可抑制艾氏瘤、沃克癌肉瘤、肉瘤45和大鼠卵巢肿瘤的生长,抑制率为76%-100%。经肠胃外给药,大鼠的半数致死量似乎为6毫克/千克,小鼠为15毫克/千克。慢性毒性研究证实呋立齐对造血、胃肠和生殖器官有损害作用。停药1-2周后毒性作用消退。

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