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Bioorg Med Chem Lett. 2005 Jun 2;15(11):2894-7.

Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.

Author information

1
The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute, La Jolla, CA 92037, USA.

Abstract

Several azaline B analogs (2-10) were synthesized and evaluated for their ability to antagonize GnRH in vitro and for duration of action in inhibiting luteinizing hormone secretion in a castrated male rat assay in vivo. Analogs, 8 (IC(50) = 1.85 nM), and 9 (IC(50) = 1.78 nM), are equipotent with azaline B (1, IC(50) = 1.36 nM) in vitro. Whereas 9 is short acting, 8 is as long acting as azaline B. Other analogs have IC(50) greater than 2.0 nM and are all short acting.

PMID:
15911275
DOI:
10.1016/j.bmcl.2005.03.085
[Indexed for MEDLINE]

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