메뉴 건너뛰기




Volumn 15, Issue 3, 2005, Pages 799-803

Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides

Author keywords

LHRH antagonist; Small molecule

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; GONADORELIN; NANOPARTICLE;

EID: 19944431992     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.10.089     Document Type: Article
Times cited : (22)

References (20)
  • 16
    • 12444316598 scopus 로고    scopus 로고
    • note
    • 3): δ 3.14-3.19 (2H, t, J = 7.4 Hz), 3.64-3.69 (2H, t, J = 7.4 Hz), 4.10-4.12 (2H, d, J = 6.2 Hz), 4.87 (1H, br s), 5.29 (2H, s), 6.88-6.93 (2H, t, J = 8.7 Hz), 7.13-7.38 (9H, m), 7.60-7.68 (2H, m), 8.21 (1H, s), 8.46-8.51 (2H, m)
  • 18
    • 12444291435 scopus 로고    scopus 로고
    • note
    • Intracellular Ca mobilization data were obtained using recombinant CHO cells transfected with human and rat LHRH receptor cDNA. The cells were preincubated with a variable concentration of test compounds for 20 min at 25°C. Fluorescence changes indicating mobilization of cytoplasmic calcium (Flu-3 AM, Molecular Probes) were measured on a FDSS-3000 machine (Hamamatsu photonics) after the stimulation with 10 nM LHRH for human receptor expressing cells and 1 nM LHRH for rat receptor expressing cells. The inhibitory effect of the compounds was calculated by comparing the Integral ratio (ratio = actual fluorescence/initial fluorescence)
  • 19
    • 12444255447 scopus 로고    scopus 로고
    • note
    • 12 were incubated with 150 pM of [125I]-D-Trp6-LHRH (Pharmacia) in the presence of various concentration of compounds in assay buffer. The total binding was defined as that measured in the absence of a competing agent. Nonspecific binding was determined in the presence of 10 μM D-Trp6-LHRH


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.