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Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors

[Display omitted] Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displ... Full description

Journal Title: Bioorganic & Medicinal Chemistry Letters 01 January 2016, Vol.26(1), pp.21-24
Main Author: Gargano, Emanuele Marco
Other Authors: Perspicace, Enrico , Carotti, Angelo , Marchais-Oberwinkler, Sandrine , Hartmann, Rolf W
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2015.11.047
Link: http://dx.doi.org/10.1016/j.bmcl.2015.11.047
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title: Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors
format: Article
creator:
  • Gargano, Emanuele Marco
  • Perspicace, Enrico
  • Carotti, Angelo
  • Marchais-Oberwinkler, Sandrine
  • Hartmann, Rolf W
subjects:
  • 17β-Hsd2
  • Osteoporosis
  • Cytotoxicity
  • Biphenyl
  • 17β-Hsd1
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ispartof: Bioorganic & Medicinal Chemistry Letters, 01 January 2016, Vol.26(1), pp.21-24
description: [Display omitted] Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displayed comparable or better inhibitory activity and selectivity, as well as a lower cytotoxic effect, compared to the reference compound A. The best compound 4 (IC50=160nM, selectivity factor=168, LD50≈25μM) turned out as new lead compound for inhibition of 17β-HSD2.
language: eng
source:
identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2015.11.047
fulltext: fulltext
issn:
  • 0960-894X
  • 0960894X
  • 1464-3405
  • 14643405
url: Link


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titleAddressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors
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description[Display omitted] Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displayed comparable or better inhibitory activity and selectivity, as well as a lower cytotoxic effect, compared to the reference compound A. The best compound 4 (IC50=160nM, selectivity factor=168, LD50≈25μM) turned out as new lead compound for inhibition of 17β-HSD2.
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[Display omitted]

Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displayed comparable or better inhibitory activity and selectivity, as well as a lower cytotoxic effect, compared to the reference compound A. The best compound 4 (IC50=160nM, selectivity factor=168, LD50≈25μM) turned out as new lead compound for inhibition of 17β-HSD2.

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abstract

[Display omitted]

Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moiety. Compounds 3, 4, 7a and 8 displayed comparable or better inhibitory activity and selectivity, as well as a lower cytotoxic effect, compared to the reference compound A. The best compound 4 (IC50=160nM, selectivity factor=168, LD50≈25μM) turned out as new lead compound for inhibition of 17β-HSD2.

pubElsevier Ltd
doi10.1016/j.bmcl.2015.11.047
lad01Bioorganic & Medicinal Chemistry Letters
date2016-01-01