Steroidal ferrocenes as potential enzyme inhibitors of the estrogen biosynthesis.

Bianka Edina Herman, János Gardi, János Julesz, Csaba Tömböly, Eszter Szánti-Pintér, Klaudia Fehér, Rita Skoda-Földes, Mihály Szécsi

Abstract readEvaluation Study

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In one paragraph

Article in Biologia futura, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

What it found

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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

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4 · The record

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5 · Who and what money

Authors and funding

8 authors.

Bianka Edina Herman1st Department of Medicine, University of Szeged, Korányi fasor 8-10, P. O. Box 427, Szeged, 6720, Hungary.

János Gardi1st Department of Medicine, University of Szeged, Korányi fasor 8-10, P. O. Box 427, Szeged, 6720, Hungary.

János Julesz1st Department of Medicine, University of Szeged, Korányi fasor 8-10, P. O. Box 427, Szeged, 6720, Hungary.

Csaba TömbölyLaboratory of Chemical Biology, Institute of Biochemistry, Biological Research Centre, Hungarian Academy of Sciences, Temesvári körút 62, P. O. Box 521, Szeged, 6726, Hungary.

Eszter Szánti-PintérDepartment of Organic Chemistry, Institute of Chemistry, University of Pannonia, Egyetem utca 10, P. O. Box 158, Veszprém, 8200, Hungary.

Klaudia FehérDepartment of Organic Chemistry, Institute of Chemistry, University of Pannonia, Egyetem utca 10, P. O. Box 158, Veszprém, 8200, Hungary.

Rita Skoda-FöldesDepartment of Organic Chemistry, Institute of Chemistry, University of Pannonia, Egyetem utca 10, P. O. Box 158, Veszprém, 8200, Hungary. skodane@almos.uni-pannon.hu.

Mihály Szécsi1st Department of Medicine, University of Szeged, Korányi fasor 8-10, P. O. Box 427, Szeged, 6720, Hungary. szecsi.mihaly@med.u-szeged.hu.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The potential inhibitory effect of diverse triazolyl-ferrocene steroids on key enzymes of the estrogen biosynthesis was investigated. Test compounds were synthesized via copper-catalyzed cycloaddition of steroidal azides and ferrocenyl-alkynes using our efficient methodology published previously. Inhibition of human aromatase, steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities was investigated with in vitro radiosubstrate incubations. Some of the test compounds were found to be potent inhibitors of the STS. A compound bearing ferrocenyl side chain on the C-2 displayed a reversible inhibition, whereas C-16 and C-17 derivatives displayed competitive irreversible binding mechanism toward the enzyme. 17α-Triazolyl-ferrocene derivatives of 17β-estradiol exerted outstanding inhibitory effect and experiments demonstrated a key role of the ferrocenyl moiety in the enhanced binding affinity. Submicromolar IC

Indexed as

11-beta-Hydroxysteroid Dehydrogenase Type 1Aromatase InhibitorsEstrogensFerrous CompoundsMetallocenesSteryl-SulfataseTriazoles11-beta-Hydroxysteroid Dehydrogenase Type 1Aromatase InhibitorsEstrogensferroceneFerrous CompoundsMetallocenesSteryl-SulfataseTriazoles17β-HSD1AromataseEstrogen biosynthesisSteroidal ferrocenesSteroid sulfatase

Identifiers

PMID34554507

DOI10.1016/j.ejmech.2015.09.038

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