| Literature DB >> 11425546 |
W T Ashton1, R M Sisco, Y T Yang, J L Lo, J B Yudkovitz, K Cheng, M T Goulet.
Abstract
The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With either a phenol or methanesulfonamide terminus on the N-aralkyl side chain, potent binding affinity to the GnRH receptor was achieved. A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary amides.Entities:
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Year: 2001 PMID： 11425546 DOI： 10.1016/s0960-894x(01)00274-8
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823