Ontology highlight
ABSTRACT:
SUBMITTER: Zhao J
PROVIDER: S-EPMC7508466 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Zhao Jian J Wang Shimiao S Han Sangdon S Kim Sun Hee SH Kusnetzow Ana Karin AK Nguyen Julie J Rico-Bautista Elizabeth E Tan Hannah H Betz Stephen F SF Scott Struthers R R Zhu Yunfei Y
Bioorganic & medicinal chemistry letters 20200711 17
Nonpeptide sst2 agonists can provide a new treatment option for patients with acromegaly, carcinoid tumors, and neuroendocrine tumors. Our medicinal chemistry efforts have led to the discovery of novel 3,4-dihydroquinazoline-4-carboxamides as sst2 agonists. This class of molecules exhibits excellent human sst2 potency and selectivity against sst1, sst3, sst4 and sst5 receptors. Leading compound 3-(3-chloro-5-methylphenyl)-6-(3-fluoro-2-hydroxyphenyl)-N,7-dimethyl-N-{[(2S)-pyrrolidin-2-yl]methyl} ...[more]