发明授权
US5053431A Derivatives of chrysophanol as topoisomerase II inhibitors
失效
chrysophanol的衍生物作为拓扑异构酶II抑制剂
- 专利标题： Derivatives of chrysophanol as topoisomerase II inhibitors
- 专利标题（中）： chrysophanol的衍生物作为拓扑异构酶II抑制剂
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申请号： US544203申请日： 1990-06-26
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公开(公告)号： US5053431A公开(公告)日： 1991-10-01
- 发明人: Kyoichi A. Watanabe , Masao Koyama , Ting-Chao Chou
- 申请人： Kyoichi A. Watanabe , Masao Koyama , Ting-Chao Chou
- 申请人地址： NY New York
- 专利权人： Sloan-Kettering Institute For Cancer Research
- 当前专利权人： Sloan-Kettering Institute For Cancer Research
- 当前专利权人地址： NY New York
- 主分类号： C07C50/34
- IPC分类号： C07C50/34 ; C07C225/24 ; C07C271/12 ; C07D295/116 ; C07D521/00
摘要：
The present invention concerns compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, a hydroxy group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a secondary amino group (NHalkyl) or a tertiary amino group (N(alkyl).sub.2); andZ is hydrogen or a halogen.The invention further provides a method of inhibiting topoisomerase II using a compound having the structure: ##STR2## wherein R.sup.1 is hydrogen, a hydroxy group or a methoxy group;R.sup.2 is hydrogen or a methyl group;R.sup.3 is hydrogen or a methyl group;Y is a halogen, secondary amino group (NHalkyl) or a tertiary amino group (N(alkyl).sub.2); andZ is hydrogen or a halogen.The invention further concerns pharmaceutical compositions which comprise the above-identified compound or the acid salts thereof, and the use of the compound or compositions for treating a malignancy in a subject.
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