申请人:Research Corporation Technologies, Inc.
公开号:US05397802A1
公开(公告)日:1995-03-14
Gem-Dichlorocyclopropanes (Analog II derivatives) which demonstrate antiproliferative activity toward MCF-7 cells, in vitro and are generally not reversed by estradiol or having intrinsic estrogenicity (except the hydroxyphenyl derivative Compound 30). In general the cyclopropane compounds have the formula: ##STR1## or any pharmaceutically acceptable salt thereof. X is selected from a group consisting of hydrogen and halogen atoms. The group R.sub.1 may be a hydrogen atom, an alkyl group, an acyl group, or an arylalkyl group. The group R.sub.2 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The group R.sub.3 may be a hydrogen atom, an alkyl group, a cycloalkyl group, a substituted aryl group or an unsubstituted aryl group. The group R.sub.4 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The R.sub.4 is absent when R.sub.3 is a cycloalkyl group having a first position carbon and a terminal position carbon bonded to the same carbon of the cyclopropane. Further, no more than any two of R.sub.2, R.sub.3 and R.sub.4 has an aryl group.
Gem-Dichlorocyclopropanes(类似物II衍生物)在体外对MCF-7细胞表现出抗增殖活性,通常不会被雌二醇逆转或具有内在的雌激素作用(除了羟基苯基衍生物化合物30)。通常,环丙烷化合物的化学式为:##STR1##或其任何药学上可接受的盐。X从氢原子和卤原子组成的一组中选择。基团R.sub.1可以是氢原子,烷基,酰基或芳基烷基。基团R.sub.2可以是氢原子,未取代的芳基或取代的芳基。基团R.sub.3可以是氢原子,烷基,环烷基,取代的芳基或未取代的芳基。基团R.sub.4可以是氢原子,未取代的芳基或取代的芳基。当R.sub.3是与环丙烷的同一碳原子相结合的第一个位置碳原子和末端位置碳原子的环烷基时,R.sub.4不存在。此外,R.sub.2,R.sub.3和R.sub.4中最多有两个基团是芳基。