HETEROCYCLIC STEROIDS .6. SYNTHESIS AND ESTROGEN-RECEPTOR BINDING AFFINITIES OF 8-AZA-11-OXASTEROIDS AND 8-AZA-11-OXA-D-HOMOSTEROIDS

CAMPAGNA, F and CAROTTI, A and CASINI, G and OTTO, AM (1995) HETEROCYCLIC STEROIDS .6. SYNTHESIS AND ESTROGEN-RECEPTOR BINDING AFFINITIES OF 8-AZA-11-OXASTEROIDS AND 8-AZA-11-OXA-D-HOMOSTEROIDS. FARMACO, 50 (2). pp. 137-141. ISSN 0014-827X,

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Abstract

A simple one-step synthesis of 8-aza-11-oxa-12,12-bis-ethoxycarbonyl-17-oxo-gonane and D-homogonane derivatives 3 was accomplished through cyclocondensation reaction of aldol adducts 1, derived from 1,3-cycloalkanediones and diethyl 2-oxo-malonate, with tosyl chloride and isoquinolines. Estrogen receptor binding studies in MCF-7 cell cultures showed no detectable competition of compounds 3 with [H-3]E(2) for binding, whereas a significant loss of E(2) binding was observed after overnight preincubation of 3.

Item Type: Article
Uncontrolled Keywords: PLASMA-MEMBRANE; ESTRADIOL; CELLS;
Depositing User: Dr. Gernot Deinzer
Last Modified: 19 Oct 2022 08:38
URI: https://pred.uni-regensburg.de/id/eprint/52759

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