期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 9, 页码 2067-2077出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm0613931
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资金
- NICHD NIH HHS [R01 HD039899-05, R01 HD039899, R01 HD019899, R01 HD019899-24, HD19899, R37 HD019899, HD039899] Funding Source: Medline
A series of acyline analogues incorporating L- and D-isomers of S-arylated/alkylated norcysteines [Ncy(R), where R is 2-naphthyl, methyl, and isopropyl] at positions 1, 4, 7, and 10 were synthesized. Some of these analogues were mono- and dioxidized to sulfoxides and sulfones. All of the analogues of acyline were screened for the antagonism of the GnRH-induced response in a reporter gene assay in HEK-293 cells expressing the human GnRH receptor. Nine of the analogues (9, 11, 15, 16, 17, 19, 20 21, and 22) had antagonistic potency (IC50 < 2 nM) similar to that of acyline (IC50 = 0.52 nM) in this assay. Selected analogues (9, 11, 15, 16, 19, and 21) were tested in vitro for their antagonism at the rat GnRH-R in a reporter gene assay as well as in an in vivo intact male rat assay. Analogues 9 and 15 were the most potent in suppressing testosterone levels.
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