Gem-dichlorocyclopropanes as antitumor agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ether doai

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514717, 514718, 514719, 514736, 568631, 568644, 568774, 568775, 568807, A61K 31045

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active

056632070

ABSTRACT:
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 he 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.

REFERENCES:
Magarian et al., "Synthesis of Cyclopropyl Analogs of Stilbene and Stilbenediol as Possible Antiestrogens", Journal of Pharmaceutical Sciences, vol. 64, No. 10, Oct. 1975, pp. 1626-1632 Oct. 1975.

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