Synthesis and biological effect of halogen substituted phenyl acetic acid derivatives of progesterone as potent progesterone receptor antagonists

Cabeza, Marisa; Bratoeff, Eugene; Gómez, Georgina; Heuze, Ivonne; Rojas, Arely; Ochoa, Martha; Palomino, Miguel A.; Revilla, C

doi:10.1016/j.jsbmb.2008.06.011

Cited by 10 publications

(2 citation statements)

References 31 publications

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“…After incubation, 0.21 mL saturated ammonium sulfate in TEMD buffer (30%) was added [20,24]. The mixture was further incubated for 1 h with occasional shaking for the precipitation of the [ 3 H] R5020-complex.…”

Section: Genementioning

confidence: 99%

Molecular interactions of natural and synthetic steroids in female hamsters’ flank organs

Cabeza

Naranjo

Heuze

et al. 2012

Journal of Dermatological Science

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Section: Genementioning

confidence: 99%

Molecular interactions of natural and synthetic steroids in female hamsters’ flank organs

Cabeza

Naranjo

Heuze

et al. 2012

Journal of Dermatological Science

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“…The competition studies reported previously in 10 showed an IC 50 value for unlabeled progesterone of 4 nM, when they used labeled promegestone at a concentration of 0.4 nM. The difference between the study of Palmer et al 10 and our study is that we could precipitate the PR with ammonium sulfate 11. This procedure permitted us to obtain a purified fraction of the PR 12 and to improve the competition analysis.…”

Section: Discussionmentioning

confidence: 56%

Biological Evaluation of Androstene Derivatives

Garrido¹,

Bratoeff²,

García-Lorenzana

et al. 2012

Archiv der Pharmazie

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The effect of several new dihydroepiandrosterone ester derivatives A2-A6 was demonstrated using female cycling mice, which were synchronized for estrus with luteinizing hormone-releasing hormone (LHRH) and injected with the steroids. The binding to the progesterone receptor (PR), was obtained from the cytosol of uteri from adult estrogen-primed rabbits. A1 binds to the PR and inhibited the ovulation in cycling mice stimulated with LHRH. The activity of the endometrium and mammary glands in these mice was markedly reduced as compared to the control. A2, A4, and A5 were not active; nevertheless, A3 binds to the PR with high affinity. However, this steroid did not produce any effect as compared to that observed for the control in the endometrial and mammary glands. A6 binds to the PR with the highest affinity and induces a synergistic activity with progesterone in these tissues. Furthermore, A6 inhibited the ovulation in the same manner as A1. These results suggested that A1 and A6 are blocking the gonadotropin secretion. A1 inhibited the conversion of progesterone to 5α-progesterone. As a result of this, a blockage of the ductal and alveolar epithelial cell proliferation in the mammary and endometrial glands, which depends on 5α-progesterone, was also observed.

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