POTENTIAL CNS ANTI-TUMOR AGENTS .6. AZIRIDINYLBENZOQUINONES-III

被引：71

作者：

DRISCOLL, JS

DUDECK, L

CONGLETON, G

GERAN, RI

机构：

[1] Drug Design and Chemistry Section, Laboratory of Medicinal Chemistry, Division of Cancer Treatment, National Cancer Institute, National Institutes of Health, Bethesda, Maryland

[2] Hazleton Laboratories, Vienna, Virginia

[3] Drug Evaluation Branch, Division of Cancer Treatment, National Cancer Institute, National Institutes of Health, Bethesda, Maryland

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 02期

关键词：

Antitumor agents; CNS—aziridinylbenzoquinones evaluated in vivo; various test systems; Aziridinylbenzoquinones—evaluated as potential CNS antitumor agents in vivo; CNS antitumor activity—aziridinylbenzoquinones evaluated in vivo; Structure‐activity relationships—aziridinylbenzoquinones evaluated as potential CNS antitumor agents in vivo;

D O I：

10.1002/jps.2600680217

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thirty‐one aziridinylbenzoquinones were compared against five murine tumor models in vivo. Two intracerebral (ependymoblastoma and L‐1210 leukemia) and three intraperitoneal (P‐388 and L‐1210 leukemia and B16 melanoma) systems were utilized. Excellent activity was observed for many compounds. Multiple long‐term survivors were produced in the ependymoblastoma, P‐388, and intraperitoneal L‐1210 systems. Diethyl 2,5‐bis(1‐aziridinyl)‐3,6‐dioxo‐1,4‐cyclohexadiene‐1,4‐dicarbamate demonstrated superior activity in all five test systems. This compound also was reproducibly active against two colon tumors, a mammary tumor, and the intracerebrally implanted P‐388 leukemia model. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：185 / 188

页数：4

共 16 条

[1] POTENTIAL CENTRAL NERVOUS-SYSTEM ANTITUMOR AGENTS - AZIRIDINYLBENZOQUINONES .2. [J].

CHOU, F ;

KHAN, AH ;

DRISCOLL, JS .

JOURNAL OF MEDICINAL CHEMISTRY, 1976, 19 (11) :1302-1308

[2]

DOMAGK G., 1954, ZEITSCHR KREBSFORSCH, V59, P617, DOI 10.1007/BF00631303

[3]

DRISCOLL JS, 1974, CANCER CHEMOTH REP 3, V4, P1

[4]

FARBENFABRIKEN BAYER, 1956, Patent No. 762723

[5]

GERAN RI, 1972, CANC CHEMOTHER REP, V3, P1

[6] STUDY ABOUT GROWTH OF 2 TUMORS OF SOLID YOSHIDA SARCOMA OF RAT IN SAME ANIMALS AS WELL AS ABOUT REACTIONS OF TUMORS OF DIFFERENT SIZES TO TREATMENT WITH 2-TRISETHYLENEIMINOBENZOCHINONE, 3-TRISETHYLENEIMINOBENZOCHINONE, 5-TRISETHYLENEIMINOBENZOCHINONE (1,4 [J].

HARTLEIB, J .

ZEITSCHRIFT FUR KREBSFORSCHUNG UND KLINISCHE ONKOLOGIE, 1974, 81 (01) :1-6

[7] POTENTIAL CENTRAL NERVOUS-SYSTEM ANTITUMOR AGENTS - AZIRIDINYLBENZOQUINONES .1. [J].

KHAN, AH ;

DRISCOLL, JS .

JOURNAL OF MEDICINAL CHEMISTRY, 1976, 19 (02) :313-317

[8] EFFECTS OF CYTOSTATIC AGENTS ON SHORT-TERM CULTURES (H-3-URIDINE INCORPORATION) AND TISSUE-CULTURES (CELL COUNTS) FROM HUMAN TUMORS [J].

MATTERN, J ;

WAYSS, K ;

VOLM, M .

ARCHIV FUR GYNAKOLOGIE, 1974, 216 (03) :273-279

[9]

MERKER PC, 1975, CANCER CHEMOTH REP 1, V59, P729

[10]

NAKAO H, 1972, CHEM PHARM BULL, V20, P1962

← 1 2 →