ANTI-NEOPLASTIC AGENTS .64. 1,4-BIS(2'-CHLOROETHYL)-1,4-DIAZABICYCLO[2.2.1]HEPTANE DIHYDROGEN DIMALEATE

被引：10

作者：

PETTIT, GR ^{[1
]}

GIESCHEN, DP ^{[1
]}

PETTIT, WE ^{[1
]}

机构：

[1] ARIZONA STATE UNIV,DEPT CHEM,TEMPE,AZ 85281

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 12期

关键词：

1,4‐Bis(2′‐chloroethyl)‐1,4‐diazabicyclo‐[2.2.1]heptane cation—antineoplastic activity, synthesis, diperchlorate and dihydrogen dimaleate salts; Antineoplastic agents—1,4‐bis(2′ ‐ chloroethyl) ‐ 1,4‐diazabicyclo[2.2.1]heptane cation, synthesis, diperchlorate and dihydrogen dimaleate salts; Heterocyclic anticancer agents— 1,4‐bis(2′‐chloroethyl)‐1,4‐diazabicyclo[2.2.1]heptane cation, synthesis, diperchlorate and dihydrogen dimaleate salts;

D O I：

10.1002/jps.2600681220

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 1,4‐bis(2′‐chloroethyl)‐1,4‐diazabicyclo[2.2.1]heptane dication (II) exhibits remarkable antineoplastic activity. Detailed evaluation of several dianion derivatives showed a curative response level against the murine P‐388 lymphocytic leukemia, colon 26, CD8F1 mammary, and the Walker 256 carcinosarcoma (rat) tumor systems. In addition, significant cancer chemotherapeutic activity was found against the murine L‐1210 lymphoid leukemia, colon 38, and B16 melanocarcinoma tumor systems. The bicyclo dication (II) first was isolated, evaluated, and stored as the diperchlorate derivative (Ila). Because of the promising anticancer activity of Ila, procedures were developed for obtaining other anion derivatives for comparative biological purposes. Several naturally occurring substances were evaluated, and the dihydrogen dimaleate derivative (IIi) obtained by an ion‐exchange technique was the most suitable. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：1539 / 1542

页数：4

共 16 条

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