Discovery of highly functionalized 5,6-<i>seco</i>-grayanane diterpenoids as potent competitive PTP1B inhibitors
Junfei Zhou, Zhili Zuo, Junjun Liu, Hanqi Zhang, Guijuan Zheng, Guangmin Yao
Abstract
Three competitive PTP1B inhibitory diterpenoids with a 5,6-<italic>seco</italic>-grayanane carbon skeleton (<bold>1–3</bold>) were isolated and identified from<italic>Rhododendron molle</italic>. A more potent competitive PTP1B inhibitor (<bold>9</bold>) was designed and prepared based on a docking study.
Topics & Concepts
ChemistryStereochemistryCarbon skeletonTerpenoidTerpeneProtein Tyrosine PhosphatasesBioactive Compounds and Antitumor AgentsCarbohydrate Chemistry and Synthesis