Characterization of Mono- and Diaminopyrimidine Derivatives as Novel, Nonpeptide Gonadotropin Releasing Hormone (GnRH) Receptor Antagonists.

ChemInform ◽  
2003 ◽  
Vol 34 (14) ◽  
Author(s):  
David R. Luthin ◽  
Yufeng Hong ◽  
et al. et al.
Keyword(s):  
Gnrh Receptor ◽  
Gonadotropin Releasing Hormone ◽  
Receptor Antagonists ◽  
Releasing Hormone

Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists

2002 ◽  
Vol 12 (24) ◽  
pp. 3635-3639 ◽  
Author(s):  
David R Luthin ◽  
Yufeng Hong ◽  
Eileen Tompkins ◽  
Kenna L Anderes ◽  
Genevieve Paderes ◽  
...  
Keyword(s):  
Gnrh Receptor ◽  
Gonadotropin Releasing Hormone ◽  
Receptor Antagonists ◽  
Releasing Hormone

scholarly journals Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor

MedChemComm ◽  
2017 ◽  
Vol 8 (10) ◽  
pp. 1965-1969 ◽  
Author(s):  
Richard Fjellaksel ◽  
Marc Boomgaren ◽  
Rune Sundset ◽  
Ira H. Haraldsen ◽  
Jørn H. Hansen ◽  
...  
Keyword(s):  
Small Molecule ◽  
Hormone Receptor ◽  
Gnrh Receptor ◽  
Gonadotropin Releasing Hormone ◽  
Synthesis And Characterization ◽  
Releasing Hormone ◽  
Gonadotropin Releasing Hormone Receptor

In this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-tert-butylphenyl)-4-piperazinyl-benzimidazole scaffold via Cu-catalysed azide alkyne cycloaddition.

Copper-Mediated Late-Stage Iodination and 123I-Labelling of Triazole-benzimidazole Bioactives

Synlett ◽  
2018 ◽  
Vol 29 (11) ◽  
pp. 1491-1495 ◽  
Author(s):  
Jørn Hansen ◽  
Richard Fjellaksel ◽  
Rune Sundset ◽  
Patrick Riss
Keyword(s):  
Late Stage ◽  
Gnrh Receptor ◽  
Gonadotropin Releasing Hormone ◽  
Receptor Antagonists ◽  
Reaction Conditions ◽  
Releasing Hormone

The copper-mediated azide-alkyne cycloaddition has been studied to achieve late-stage introduction of iodine onto novel triazole-benzimidazole Gonadotropin Releasing Hormone (GnRH)-receptor antagonists. Moreover, the reaction conditions can affect a direct regioselective C–H iodination of the benzimidazole, leading to a range of novel iodo-analogues. The methodologies are powerful strategies for late-stage 123I-labelling of complex bioactives. Our investigations have generated two highly promising 123I-labelled radiotracer candidates that retain high affinities for the GnRH-receptor.

The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists

2002 ◽  
Vol 12 (23) ◽  
pp. 3467-3470 ◽  
Author(s):  
David R. Luthin ◽  
Yufeng Hong ◽  
Ved P. Pathak ◽  
Genevieve Paderes ◽  
Karen D. Nared-Hood ◽  
...  
Keyword(s):  
Small Molecule ◽  
Gnrh Receptor ◽  
Gonadotropin Releasing Hormone ◽  
Receptor Antagonists ◽  
Releasing Hormone
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