ArticleRSC medicinal chemistry2024
On-resin synthesis of Lanreotide epimers and studies of their structure-activity relationships.
Article in RSC medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Peptide drugs often accompany epimeric impurities (isomers). Therefore, efficient chemical synthesis of epimers is critical to identify them correctly and investigate their biological activities. Here, we report the rapid synthesis and structure-activity relationship (SAR) studies of eight possible epimers of a somatostatin synthetic analog (SSA), lanreotide (LAN). SPPS and the subsequent on-resin rapid disulfide closure method offered >90% conversion yield for all epimers (P1-P8). Further, we developed an analytical method to separate these epimers, which enabled the profiling of five epimeric impurities in the API, purchased for Somatuline generic formulations. In SAR studies, most LAN epimers revealed compromised antiproliferative activity, while the P7 epimer retained antiproliferative activity similar to LAN API, as supported by
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