SYNTHESIS AND PRELIMINARY EVALUATION OF AGENTS INCORPORATING THE PHARMACOPHORE OF THE DUOCARMYCIN PYRINDAMYCIN ALKYLATION SUBUNIT - IDENTIFICATION OF THE CC-1065 DUOCARMYCIN COMMON PHARMACOPHORE

被引:136
作者
BOGER, DL [1 ]
ISHIZAKI, T [1 ]
ZARRINMAYEH, H [1 ]
KITOS, PA [1 ]
SUNTORNWAT, O [1 ]
机构
[1] UNIV KANSAS,DEPT BIOCHEM,LAWRENCE,KS 66045
关键词
D O I
10.1021/jo00302a002
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
: The synthesis of 7 (CI-TMI) incorporating the parent l,2,7,7a-tetrahydrocycloprop[l,2-c]indol-4-one (Cl) alkylation subunit of duocarmycin is described. The results of its comparative evaluation (in vitro cytotoxic activity, DNA covalent alkylation properties) illustrate that 7 (CI-TMI) constitutes an agent bearing the minimum potent pharmacophore of the duocarmycin alkylation subunit and the common pharmacophore of the duocarmycin/CC-1065 alkylation subunits. © 1990, American Chemical Society. All rights reserved.
引用
收藏
页码:4499 / 4502
页数:4
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