Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1993-02-22
1995-03-14
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514717, 514736, 560130, 568635, 568639, 568647, 568774, 568775, 568807, A01N 3702
Patent
active
053978021
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 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.
REFERENCES:
Madeddu et al., "A New Method for Evaluating the Inhibiting Potency of Antiestrogens on Breast Cancer Cell Lines", Anticancer Research, 6: 11-16, (1986).
Griffin et al., "Synthesis and Biological Evaluation of a Series of Gem-Dichlorocyclopropanes as Antitumor Agents", Anti-Cancer Drug Design, 7: 49-66, (1992).
Hausser et al., J. Org. Chem., 37:4087-4090, (1972).
Magarian et al., J. Pharmaceutical Sciences, 61: 1216-1219, (1972).
Magarian et al, J. Pharmaceutical Sciences, 64:1626-1632, (1975).
Griffin May T.
Magarian Robert A.
Pento Joseph T.
Dees Jos,e G.
Jones Dwayne C.
Research Corporation Technologies Inc.
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