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1,3,3,5,5-五氮杂环庚三烯-1-硫代-2,4,6-三氮杂-3,5-二磷杂环庚三烯-1-氧化物(一种新型无机环抗肿瘤剂)对多种实验性肿瘤的作用

Effect of 1,3,3,5,5-pentaziridino-1-thia-2,4,6-triaza-3,5-diphosphorine-1-oxide, a new antitumor agent with inorganic ring, on various experimental tumors.

作者信息

Kitazato K, Takeda S, Unemi N

出版信息

J Pharmacobiodyn. 1982 Oct;5(10):803-10. doi: 10.1248/bpb1978.5.803.

Abstract

1,3,3,5,5-Pentaziridino-1-thia-2,4,6-triaza-3,5-diphosphorine-1-oxide (SOAz), a new antitumor agent, was evaluated for antitumor activity against various mouse- and rat-tumor systems. The optimal treatment regimens of SOAz (i.p.) gave 262% and 134% increase in life span (ILS) in mice with P388 leukemia and L1210 leukemia implanted intraperitoneally, respectively, and 239% ILS in rats with Yoshida sarcoma of which 86% survived for 60 d after intraperitoneal tumor implantation. The compound showed a definite activity against Lewis lung carcinoma implanted intravenously. The compound also exhibited 80-100% inhibition of tumor local growth in all of four experimental tumor systems used in the present study. In contrast to cyclophosphamide, SOAz was active against B16 melanoma and Meth A, and demonstrated high activity against a subline of L1210 leukemia resistant to cyclophosphamide.

摘要

1,3,3,5,5-五氮丙啶基-1-硫杂-2,4,6-三氮杂-3,5-二磷杂环庚烷-1-氧化物(SOAz)是一种新型抗肿瘤药物,对多种小鼠和大鼠肿瘤系统的抗肿瘤活性进行了评估。SOAz腹腔注射的最佳治疗方案使腹腔内植入P388白血病和L1210白血病的小鼠的生存期分别延长了262%和134%,使植入吉田肉瘤的大鼠的生存期延长了239%,其中86%的大鼠在腹腔内植入肿瘤后存活了60天。该化合物对静脉注射植入的Lewis肺癌有明确的活性。在本研究使用的所有四个实验肿瘤系统中,该化合物还对肿瘤局部生长表现出80%-100%的抑制作用。与环磷酰胺不同,SOAz对B16黑色素瘤和Meth A有活性,并对耐环磷酰胺的L1210白血病亚系表现出高活性。

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