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- W2950403151 abstract "In order to develop cytotoxic estrogens with a specific effect on hormone-dependent mammary tumors, two 1,1,2-triphenylbut-1-enes with a 4-OH group at one C-1-phenyl ring and a chloro-[4] or bromo-[8] anilin mustard moiety at the other C-1-phenyl ring were synthesized. 4 and 8 exerted strong alkylating activity and an irreversible binding to the estrogen receptor. In spite of relatively low receptor affinities, both anilin mustards exhibited a better effect on a receptor-positive breast cancer cell line as well as on a hormone-dependent mammary carcinoma of the mouse than on a receptor-negative cell line and a hormone-independent mammary carcinoma. Therefore, a selective antitumor activity of 4 and 8 is likely.Cytotoxische Ostrogene: Anilin-Lost verknupfte 1,1,2-Triphenyl-but-1-ene mit mammatumorhemmender WirkungZur Entwicklung cytotoxischer Ostrogene mit einer spezifischen Wirkung auf hormonabhangige Mammacarcinome wurden zwei 1,1,2-Triphenylbut-1-ene mit einer 4-OH Gruppe an einem C-1-Phenylrest und einem Chlor-[4] bzw. Brom-[8]-anilinlost-Rest am 2. C-1-Phenylrest synthetisiert. 4 und 8 zeigten starke alkylierende Aktivitat und banden irreversibel an den Ostrogenrezeptor. Trotz ihrer relativ geringen Rezeptoraffinitaten wiesen beide Anilinlost-Derivate eine bessere Wirkung an einer rezeptorpositiven Brustkrebszellinie und an einem hormonabhangigen Mammacarcinom der Maus auf als an einer rezeptornegativen Zellinie und einem hormonunabhangigen Mammacarcinom. Daher ist eine selektive Antitumorwirkung von 4 und 8 anzunehmen." @default.
- W2950403151 created "2019-06-27" @default.
- W2950403151 creator A5016806175 @default.
- W2950403151 creator A5062265459 @default.
- W2950403151 date "1989-07-04" @default.
- W2950403151 modified "2023-10-14" @default.
- W2950403151 title "ChemInform Abstract: Cytotoxic Estrogens: Anilin Mustard-Linked 1,1,2-Triphenylbut-1-enes with Mammary Tumor Inhibiting Activity." @default.
- W2950403151 cites W2081879315 @default.
- W2950403151 doi "https://doi.org/10.1002/chin.198927147" @default.
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