메뉴 건너뛰기




Volumn 16, Issue 18, 2006, Pages 4959-4964

Newly discovered orally active pure antiestrogens

Author keywords

Carboxy moiety; estrogen receptor; Pure antiestrogen; Steroid scaffold

Indexed keywords

ANTIESTROGEN; CH 4893237; STEROID; UNCLASSIFIED DRUG;

EID: 33746829967     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.06.047     Document Type: Article
Times cited : (13)

References (28)
  • 10
    • 33746831334 scopus 로고    scopus 로고
    • Jo, J. C.; Kwon, H. A.; Lim, H. S.; Choi, J. Y.; Morikawa, K.; Kanbe, Y.; Nishimoto, M.; Kim, M. H.; Nishimura, Y. Eur. Pat. Appl. EP1241158, 2002.
  • 11
    • 33746799473 scopus 로고    scopus 로고
    • Nabuchi, Y.; Araya, H.; Kawata, S.; Morikawa, K.; Kanbe, Y.; Ohtake, Y.; Kaiho, S.; Taniguchi, K.; Tsunenari, T.; Takasu, H. Eur. Pat. Appl. EP1491551, 2004.
  • 12
    • 33746813755 scopus 로고    scopus 로고
    • note
    • ® AD column with the eluent, hexane/isopropanol/AcOH, 980:20:1. The (-)-isomer was first eluted, and the (+)-isomer used in Scheme 3 was eluted second.
  • 13
    • 33746789559 scopus 로고    scopus 로고
    • note
    • Antiestrogen activity was determined as anti-uterotrophic effect of the test compound in ovariectomized (OVX) mice. OVX mice were treated with 0.1 μg of 17β-estradiol benzoate in peanut oil solution subcutaneously along with the indicated dose of the test compound in 5% gum arabic-water suspension orally once a day for three consecutive days. Approximately 24 h after the last administration, mice were euthanized, and their uterine weights were measured. Antiestrogen activity, determined by percent inhibition of estrogen-stimulated uterine weight gain by the test compound, was calculated according to the following equation: % inhibition = 100 × (1 - (T - C)/(E - C)). Estrogen activity was determined as uterotrophic effect of the test compound in OVX mice. OVX mice were treated with the indicated dose of the test compound in 10% EtOH-peanut oil solution subcutaneously once a day for three consecutive days. Approximately 24 h after the last administration, mice were euthanized, and their uterine weights were measured. Estrogen activity, determined by percent uterine weight gain by the test compound, was calculated according to the following equation: % uterine weight gain = 100 × (T - C)/(E - C). T, E, and C refer to uterine weight gain per body weight by the test compound, by 17β-estradiol benzoate, and by vehicle, respectively.
  • 14
    • 33746825620 scopus 로고    scopus 로고
    • note
    • The RBA value for ICI182,780 we obtained appears higher than other published values, which may be due to the experimental condition. The condition we used mainly differs from other reports in that the temperature we used is 25 °C, whereas the temperature other reports used is 0 or 4 °C. We speculate that ER degradation by ICI182,780 at 25 °C proceeded faster than at 0 or 4 °C, which led to high RBA value for ICI182,780 compared to those reported in the literature.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.