39931-87-8Relevant articles and documents
Synthesis of Norgestomet and its 17β-isomer and evaluation of their agonistic activities against progesterone receptor
Kurohara, Takashi,Ito, Takahito,Tsuji, Genichiro,Misawa, Takashi,Yokoo, Hidetomo,Yanase, Yuta,Shoda, Takuji,Sakai, Takatoshi,Hosoe, Junko,Uchiyama, Nahoko,Akiyama, Hiroshi,Demizu, Yosuke
supporting information, (2021/10/04)
Norgestomet is a synthetic progesterone derivative applied in veterinary medicine to control estrus and ovulation in cattle. Norgestomet has been widely used in the livestock industry to promote the synchronization of estrus in cattle and increase pregnancy rates. However, highly reproducible synthetic methods for Norgestomet have been rarely reported. Here, we described a method for the synthesis of Norgestomet and performed quantitative NMR analysis to determine the purity of the products. Moreover, the agonistic activity of the synthesized compounds against progesterone receptors (PRs) was evaluated using an alkaline phosphatase assay. We synthesized Norgestomet with 97.9% purity that exhibited agonistic activity against PR with EC50 values of 4.5 nM. We also synthesized the 17β-isomer of Norgestomet with 92.7% purity that did not exhibit any PR agonistic activity. The proposed synthetic route of Norgestomet can facilitate the assessment of residual Norgestomet in foods.
Design and synthesis of fluorescently labeled steroidal antiestrogens
Hanson, Robert N.,Gajadeera, Nisal
, p. 39 - 46 (2019/02/28)
A set of derivatives of 11β-(4-oxyphenyl)estradiol were prepared as potential fluorescent imaging agents for the evaluation of the estrogen receptor. The compounds were designed based on the established affinity and selectivity of 11β-[4-(dimethylethoxy)p
Synthesis and biological evaluation of 11′ imidazolyl antiprogestins and mesoprogestins
Nickisch, Klaus,Elger, Walter,Santhamma, Bindu,Garfield, Robert,Killeen, Zachary,Amelkina, Olga,Schneider, Birgitt,Meister, Reinhard
, p. 45 - 55 (2014/12/11)
Antiprogestins with a 4′ para imidazolylphenyl moiety were synthesized and their biochemical interactions with the progesterone and glucocorticoid receptor were investigated. Depending on the substitution pattern at the 17 position partial progesterone re