Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed
along with the surprising use property of these compounds as a anti-tumor
agents in humans against breast carcinoma, which include:
2-(N'-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid
methyl ester (OF-06),
1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihyd
ro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07),
4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10),
4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl
ester (3F-11),
2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid
(3F-15), and
4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one
(3F-16) as well as some novel derivatives of these compounds claimed (see
Table 2). The invention also encompasses a class of the compounds with the
novel property of anti-tumor activity against human breast cancer, which
includes the following compounds
4-(4-Ethoxy-phenyl)-2-(N'-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-but
yric acid methyl ester (OF-13);
2-{N'-[1-(4-Chloro-phenyl)-ethylidene]-hydrazino}-4-oxo-4-phenyl-but-2-eno
ic acid methyl ester (OF-20);
2-(N'-Fluoren-9-ylidene-hydrazino)-4-oxo-4-phenyl-but-2-enoic acid methyl
ester (1F-04); and
4-Chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic
acid methyl ester (3F-19).
Mittel der Kategorie der Säurederivate 4-oxo-butenoic werden zusammen mit der überraschenden Gebraucheigenschaft dieser Mittel als Antitumormittel in den Menschen gegen Brustkrebsgeschwür freigegeben, die einschließen: saurer Methylester 2-(N'-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic (OF-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihyd ro-1H-pyrrole-2-carboxylic saurer Methylester (1F-07), Säure 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric (3F-10), saurer Ethylester 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric (3F-11), Säure 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic (3F-15) und 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) sowie einige Romanableitungen dieser Mittel behauptet (sehen Sie Tabelle 2). Die Erfindung gibt auch eine Kategorie Mittel mit der Romaneigenschaft der Antitumortätigkeit gegen menschlichen Brustkrebs um, der den folgenden yric sauren Methylester der Mittel 4-(4-Ethoxy-phenyl)-2-(N'-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-but (OF-13) miteinschließt; 2-{N'-[1-(4-Chloro-phenyl)-ethylidene]-hydrazino}-4-oxo-4-phenyl-but-2-eno saurer Methylester der IS (OF-20); saurer Methylester 2-(N'-Fluoren-9-ylidene-hydrazino)-4-oxo-4-phenyl-but-2-enoic (1F-04); und saurer Methylester 4-Chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic (3F-19).
