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Volumn 14, Issue 2, 2004, Pages 187-199

Recent advances in small molecule gonadotrophin-releasing hormone receptor antagonists

Author keywords

Gonadotrophin releasing hormone (GnRH) receptor; Small molecule antagonist

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; BENZOTHIAZOLE DERIVATIVE; GONADORELIN AGONIST; GONADORELIN ANTAGONIST; GONADORELIN RECEPTOR; GUANIDINE DERIVATIVE; INDOLE DERIVATIVE; PEPTIDE HORMONE ANTAGONIST; PYRIMIDINONE DERIVATIVE; PYRROLOPYRIMIDINE DERIVATIVE; QUINOLINE DERIVATIVE; SUFUGOLIX; UNCLASSIFIED DRUG;

EID: 1242352550     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.14.2.187     Document Type: Review
Times cited : (16)

References (24)
  • 2
    • 0028285865 scopus 로고
    • Gonadotrophin-releasing hormone agonists. A guide to use and selection
    • [Erratum in Drugs (1994) 48:326]
    • FILICORI M: Gonadotrophin-releasing hormone agonists. A guide to use and selection. Drugs (1994) 48:41-58 [Erratum in Drugs (1994) 48:326].
    • (1994) Drugs , vol.48 , pp. 41-58
    • Filicori, M.1
  • 3
    • 0028235123 scopus 로고
    • The use of luteinising hormone releasing hormone agonist and antagonists in gynaecological cancers
    • EMONS G, SCHALLY AV: The use of luteinising hormone releasing hormone agonist and antagonists in gynaecological cancers. Hum. Reprod. (1994) 9:1364-1379.
    • (1994) Hum. Reprod. , vol.9 , pp. 1364-1379
    • Emons, G.1    Schally, A.V.2
  • 4
    • 0026098581 scopus 로고
    • Gonadotrophin-releasing hormone and its analogues
    • CONN PM, CROWLEY WF: Gonadotrophin-releasing hormone and its analogues. N. Engl. J. Med. (1991) 324:93-103.
    • (1991) N. Engl. J. Med. , vol.324 , pp. 93-103
    • Conn, P.M.1    Crowley, W.F.2
  • 5
    • 0344444706 scopus 로고    scopus 로고
    • Gonadotrophin-releasing hormone antagonists
    • HERBST KL: Gonadotrophin-releasing hormone antagonists. Curr. Opin. Pharmacol. (2003) 3:660-666.
    • (2003) Curr. Opin. Pharmacol. , vol.3 , pp. 660-666
    • Herbst, K.L.1
  • 7
    • 0037413559 scopus 로고    scopus 로고
    • Discovery of a thieno [2,3-d] pyrimidine-2.4-dione bearing a p-methoxyureidophenyl moiety at the position 6: A highly potent and orally bioavailable non-peptide antagonist for human luteinising hormone-releasing hormone receptor
    • SASAKI S, CHO N, NARA Y et al.: Discovery of a thieno [2,3-d] pyrimidine-2.4-dione bearing a p-methoxyureidophenyl moiety at the position 6: a highly potent and orally bioavailable non-peptide antagonist for human luteinising hormone-releasing hormone receptor. J. Med. Chem. (2003) 46:113-124.
    • (2003) J. Med. Chem. , vol.46 , pp. 113-124
    • Sasaki, S.1    Cho, N.2    Nara, Y.3
  • 8
    • 0038021571 scopus 로고    scopus 로고
    • Suppression of a pituitary-ovarian axis by chronic oral administration of a novel non-peptide gonadotriphin-releasing hormone antagonist, TAK-013, in cynomolgus monkeys
    • HARA T, ARAKI H, KUSAKA M et al.: Suppression of a pituitary-ovarian axis by chronic oral administration of a novel non-peptide gonadotriphin-releasing hormone antagonist, TAK-013, in cynomolgus monkeys. J. Clin. Endocrinol. Metab. (2003) 88:1697-1704.
    • (2003) J. Clin. Endocrinol. Metab. , vol.88 , pp. 1697-1704
    • Hara, T.1    Araki, H.2    Kusaka, M.3
  • 9
    • 1242336514 scopus 로고    scopus 로고
    • Effect of single dose of TAK-013, a new non-peptide orally active gonadotrophin-releasing hormone antagonist, in healthy young men
    • CLARK E, BOYCE M, WARRINGTON S et al.: Effect of single dose of TAK-013, a new non-peptide orally active gonadotrophin-releasing hormone antagonist, in healthy young men. Proc. Br. Pharmacol. Soc. Clin. Pharmacol. Section, Br. J Clin. Pharmacol. (2003) 55:443.
    • (2003) Proc. Br. Pharmacol. Soc. Clin. Pharmacol. Section, Br. J Clin. Pharmacol. , vol.55 , pp. 443
    • Clark, E.1    Boyce, M.2    Warrington, S.3
  • 10
    • 18444369293 scopus 로고    scopus 로고
    • A new class of potent non-peptide luteinising hormone-releasing hormone (LHRH) antagonists: Design and synthesis of 2-phenylimidazo [1,2-a] pyrimidin-5-ones
    • SASAKI S, IMAEDA T, HAYASE Y et al.: A new class of potent non-peptide luteinising hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo [1,2-a] pyrimidin-5-ones. Bioorg. Med. Chem. Lett. (2002) 12:2073-2077.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 2073-2077
    • Sasaki, S.1    Imaeda, T.2    Hayase, Y.3
  • 11
    • 0035833042 scopus 로고    scopus 로고
    • Potent non-peptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus
    • ASHTON WT, SISCO RM, YANG YT et al.: Potent non-peptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus. Bioorg. Med. Chem. Lett. (2001) 11:1727-1731.
    • (2001) Bioorg. Med. Chem. Lett. , vol.11 , pp. 1727-1731
    • Ashton, W.T.1    Sisco, R.M.2    Yang, Y.T.3
  • 12
    • 0037060924 scopus 로고    scopus 로고
    • 2-Arylindoles as gonadotrophin releasing hormone (GnRH) antagonists: Optimisation of the tryptamine side chain
    • YOUNG JR, HUANG SX, WALSH TF et al.: 2-Arylindoles as gonadotrophin releasing hormone (GnRH) antagonists: optimisation of the tryptamine side chain. Bioorg. Med. Chem. Lett. (2002) 12:827-832.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 827-832
    • Young, J.R.1    Huang, S.X.2    Walsh, T.F.3
  • 13
    • 17944383430 scopus 로고    scopus 로고
    • Orally bioavailable indole-based non-peptide GnRH receptor antagonists with high potency and functional activity
    • ASHTON WT, SISCO RM, KIECZYKOWSKI GR et al.: Orally bioavailable indole-based non-peptide GnRH receptor antagonists with high potency and functional activity. Bioorg. Med. Chem. Lett. (2001) 11:2597-2602.
    • (2001) Bioorg. Med. Chem. Lett. , vol.11 , pp. 2597-2602
    • Ashton, W.T.1    Sisco, R.M.2    Kieczykowski, G.R.3
  • 14
    • 0035833079 scopus 로고    scopus 로고
    • Substituted indole-5-carboxamides and -acetamides as potent non-peptide GnRH receptor antagonists
    • ASHTON WT, SISCO RM, YANG YT et al.: Substituted indole-5-carboxamides and -acetamides as potent non-peptide GnRH receptor antagonists. Bioorg. Med. Chem. Lett. (2001) 11:1723-1726.
    • (2001) Bioorg. Med. Chem. Lett. , vol.11 , pp. 1723-1726
    • Ashton, W.T.1    Sisco, R.M.2    Yang, Y.T.3
  • 15
    • 0034618152 scopus 로고    scopus 로고
    • Quinolones as gonadotrophin-releasing hormone (GnRH) antagonists: Simultaneous optimisation of the C(3)-aryl and C(6)-substituents
    • YOUNG JR, HUANG SX, CHEN I et al.: Quinolones as gonadotrophin-releasing hormone (GnRH) antagonists: simultaneous optimisation of the C(3)-aryl and C(6)-substituents. Bioorg. Med. Chem. Lett. (2000) 10:1723-1727.
    • (2000) Bioorg. Med. Chem. Lett. , vol.10 , pp. 1723-1727
    • Young, J.R.1    Huang, S.X.2    Chen, I.3
  • 16
    • 0035866652 scopus 로고    scopus 로고
    • 1H]-quinolone antagonist for the gonadotrophin-releasing hormone receptor
    • 1H]-quinolone antagonist for the gonadotrophin-releasing hormone receptor. J. Med. Chem. (2001) 44:917-922.
    • (2001) J. Med. Chem. , vol.44 , pp. 917-922
    • Devita, R.J.1    Walsh, T.F.2    Young, J.R.3
  • 17
    • 18244406324 scopus 로고    scopus 로고
    • Initial structure-activity relationship studies of a novel series of pyrrolo [1,2-a] pyrimid-7-ones as GNRH receptor antagonists
    • ZHU YF, STRUTHERS RS, CONNORS PJ et al.: Initial structure-activity relationship studies of a novel series of pyrrolo [1,2-a] pyrimid-7-ones as GNRH receptor antagonists. Bioorg. Med. Chem. Lett. (2002) 12:399-402.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 399-402
    • Zhu, Y.F.1    Struthers, R.S.2    Connors, P.J.3
  • 18
    • 0037464459 scopus 로고    scopus 로고
    • Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl imidazolo [1,2-a)pyrimid-5ones as potent GnRH receptor antagonists
    • ZHU YF, GUO Z, GROSS TD et al.: Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl imidazolo [1,2-a)pyrimid-5ones as potent GnRH receptor antagonists. J. Med. Chem. (2003) 46:1769-1772.
    • (2003) J. Med. Chem. , vol.46 , pp. 1769-1772
    • Zhu, Y.F.1    Guo, Z.2    Gross, T.D.3
  • 19
    • 0038587497 scopus 로고    scopus 로고
    • Identification of 1-arylmethyl-3-(2-aminoethyl)-5-aryluracil as novel gonadotrophin-releasing hormone receptor antagonists
    • ZHU YF, GROSS TD, GUO Z et al.: Identification of 1-arylmethyl-3-(2-aminoethyl)-5-aryluracil as novel gonadotrophin-releasing hormone receptor antagonists. J. Med. Chem. (2003) 46:2023-2026.
    • (2003) J. Med. Chem. , vol.46 , pp. 2023-2026
    • Zhu, Y.F.1    Gross, T.D.2    Guo, Z.3
  • 20
    • 10744221847 scopus 로고    scopus 로고
    • Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists
    • GUO Z, ZHU YF, TUCCI FC et al.: Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists. Bioorg. Med. Chem. Lett. (2003) 13:3311-3315.
    • (2003) Bioorg. Med. Chem. Lett. , vol.13 , pp. 3311-3315
    • Guo, Z.1    Zhu, Y.F.2    Tucci, F.C.3
  • 21
    • 18644378190 scopus 로고    scopus 로고
    • The discovery of novel small molecule non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonists
    • LUTHIN DR, HONG Y, PATHAK VP et al.: The discovery of novel small molecule non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonists. Bioorg. Med. Chem. Lett. (2002) 12:3467-3470.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 3467-3470
    • Luthin, D.R.1    Hong, Y.2    Pathak, V.P.3
  • 22
    • 18744366904 scopus 로고    scopus 로고
    • Characterization of mono- and diaminopyrimidine derivatives as novel, non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonists
    • LUTHIN DR, HONG Y, TOMPKINS E et al.: Characterization of mono- and diaminopyrimidine derivatives as novel, non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonists. Bioorg. Med. Chem. Lett. (2002) 12:3635-3639.
    • (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 3635-3639
    • Luthin, D.R.1    Hong, Y.2    Tompkins, E.3
  • 23
    • 0037405120 scopus 로고    scopus 로고
    • Biological characterization of a novel, orally active small molecule gonadotrophin-releasing hormone (GnRH) antagonist using castrated and intact rats
    • ANDERES KL, LUTHIN DR, CASTILLO R et al.: Biological characterization of a novel, orally active small molecule gonadotrophin-releasing hormone (GnRH) antagonist using castrated and intact rats. J. Pharma. Exp. Therap. (2003) 305:688-695.
    • (2003) J. Pharma. Exp. Therap. , vol.305 , pp. 688-695
    • Anderes, K.L.1    Luthin, D.R.2    Castillo, R.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.