The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 15006412 |
16 |
Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A. |
Abbott Laboratories |
| 25516782 |
8 |
GnRH antagonists: the promise of treating sex-hormone-related diseases. |
Therachem Research Medilab (India) |
| 24613701 |
6 |
Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression. |
Norwegian Medical Cyclotron Centre |
| 24018188 |
4 |
Influences of hydrocarbon linkers on the receptor binding affinities of gonadotropin-releasing hormone peptides. |
University of New Mexico |
| 17517510 |
24 |
Synthesis and evaluation of homo-bivalent GnRHR ligands. |
Leiden University |
| 22967796 |
8 |
Enhanced cellular uptake and in vitro antitumor activity of short-chain fatty acid acylated daunorubicin-GnRH-III bioconjugates. |
TBA |
| 14971889 |
50 |
Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues. |
Abbott Laboratories |
| 23031649 |
4 |
The therapeutic journey of benzimidazoles: a review. |
Punjabi University |
| 18442905 |
25 |
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers. |
Neurocrine Biosciences |
| 18282756 |
35 |
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core. |
Leiden University |
| 17920281 |
16 |
The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies. |
Neurocrine Biosciences |
| 16789738 |
61 |
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. |
Takeda Pharmaceutical |
| 16759096 |
31 |
Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III. |
Salk Institute |
| 16033265 |
33 |
Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II. |
Salk Institute |
| 14971906 |
74 |
Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists. |
Neurocrine Biosciences |
| 12502365 |
41 |
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. |
Takeda Chemical Industries |
| 11462984 |
64 |
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. |
Ferring Research Institute |
| 9784092 |
15 |
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. |
Takeda Chemical Industries |
| 21657270 |
61 |
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor. |
Takeda Pharmaceutical |
| 21395312 |
42 |
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2. |
Merck Research Laboratories |
| 20236823 |
41 |
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor. |
Wyeth Research |
| 19271735 |
35 |
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). |
Wyeth Research |
| 19251413 |
64 |
Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template. |
Wyeth Research |
| 19006286 |
37 |
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. |
Neurocrine Biosciences |
| 18667310 |
49 |
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties. |
Neurocrine Biosciences |
| 18511284 |
64 |
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor. |
Wyeth Research |
| 18442910 |
53 |
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity. |
Neurocrine Biosciences |
| 18419112 |
63 |
Non-peptide gonadotropin-releasing hormone receptor antagonists. |
Neurocrine Biosciences |
| 17937987 |
83 |
Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor. |
Astrazeneca |
| 17561404 |
59 |
Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists. |
Neurocrine Biosciences |
| 17521908 |
66 |
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists. |
Neurocrine Biosciences |
| 17402723 |
30 |
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives. |
Salk Institute |
| 17034124 |
140 |
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling. |
Neurocrine Biosciences |
| 16722655 |
28 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
Pfizer |
| 16420049 |
355 |
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
Neurocrine Biosciences |
| 15951171 |
39 |
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists. |
Neurocrine Biosciences |
| 15911275 |
20 |
Synthesis, in vivo and in vitro biological activity of novel azaline B analogs. |
Salk Institute |
| 15863308 |
28 |
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers. |
Neurocrine Biosciences |
| 15837306 |
92 |
Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives. |
Kyoto 619-0216 |
| 15715483 |
88 |
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization. |
Neurocrine Biosciences |
| 15713397 |
12 |
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists. |
Neurocrine Biosciences |
| 15664861 |
44 |
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides. |
Kyoto 619-0216 |
| 15664860 |
44 |
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides. |
Kyoto 619-0216 |
| 15664839 |
11 |
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists. |
Neurocrine Biosciences |
| 15482932 |
32 |
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists. |
Merck Research Laboratories |
| 15341961 |
31 |
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5. |
Neurocrine Biosciences |
| 15214774 |
28 |
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor. |
Neurocrine Biosciences |
| 15081023 |
26 |
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists. |
Neurocrine Biosciences |
| 15026074 |
16 |
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists. |
Merck |
| 14505682 |
29 |
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists. |
Neurocrine Biosciences |
| 12951117 |
31 |
Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor. |
Neurocrine Biosciences |
| 12951116 |
30 |
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists. |
Neurocrine Biosciences |
| 12747774 |
17 |
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists. |
Neurocrine Biosciences |
| 12699396 |
28 |
Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. |
Neurocrine Biosciences |
| 12443792 |
51 |
Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists. |
Agouron Pharmaceuticals |
| 12419391 |
8 |
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists. |
Neurocrine Biosciences |
| 12419385 |
48 |
The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists. |
Agouron Pharmaceuticals |
| 12392744 |
36 |
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists. |
Merck Research Laboratories |
| 12127533 |
23 |
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. |
Neurocrine Biosciences |
| 12127532 |
22 |
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. |
Neurocrine Biosciences |
| 12127507 |
11 |
A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones. |
Takeda Chemical Industries |
| 11859012 |
86 |
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain. |
Merck Research Laboratories |
| 11814807 |
30 |
A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists. |
Neurocrine Biosciences |
| 11814806 |
39 |
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists. |
Neurocrine Biosciences |
| 11551758 |
58 |
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity. |
Merck Research Laboratories |
| 11425547 |
137 |
Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus. |
Merck Research Laboratories |
| 11327594 |
26 |
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists. |
Merck Research Laboratories |
| 11327593 |
16 |
2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor. |
Merck Research Laboratories |
| 11300873 |
8 |
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor. |
Merck Research Laboratories |
| 10937733 |
70 |
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents. |
Merck Research Laboratories |
| 27608177 |
202 |
Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. |
Sk Chemicals |
| 10743944 |
68 |
Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides. |
Merck Research Laboratories |
| 10715150 |
5 |
Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling. |
Salk Institute |
| 30716713 |
5 |
Development of bioactive gemcitabine-D-Lys |
University of Ioannina |
| 29335207 |
52 |
Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists. |
Tiumbio |
| 1280300 |
7 |
Gonadotropin-releasing hormone antagonists with N omega-triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6. |
Salk Institute |
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