ERGOT ALKALOIDS - SYNTHESIS OF NITROSOUREA DERIVATIVES OF ERGOLINES AS POTENTIAL ANTI-CANCER AGENTS

被引:11
作者
CRIDER, AM
LU, CKL
FLOSS, HG
CASSADY, JM
CLEMENS, JA
机构
[1] PURDUE UNIV,SCH PHARM & PHARMACAL SCI,DEPT MED CHEM & PHARMACOGNOSY,W LAFAYETTE,IN 47907
[2] ELI LILLY & CO,LILLY RES LAB,INDIANAPOLIS,IN 46206
关键词
D O I
10.1021/jm00187a008
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Nitrosourea derivatives of ergolines have been synthesized for the purpose of obtaining agents with both prolactinand tumor-inhibitory activity. Two derivatives of 8-amino-6-methylergoline (3), 8-[3-(2-chloroethyl)-3-nitrosoureido]-l-nitroso-6-methylergoline (5c) and 8-[3-(2-chloroethyl)-3-nitrosoureido]-6-methylergoline (5a), have been prepared. In addition, nitroso (7) and chloroethylcarbamyl (8) derivatives of elymoclavine (6) are reported. Compounds 5a and 5c have activity against 1, 1210 leukemia in mice hut onh moderate prolactin-inhibiting activity. The chloroethylcarbamyl derivative 8 of elymoclavine is a potent prolactin inhibitor. © 1979, American Chemical Society. All rights reserved.
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页码:32 / 35
页数:4
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