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- Title
From Natural Product-Inspired Pyrrolidine Scaffolds to the Development of New Human Golgi α-Mannosidase II Inhibitors.
- Authors
Cheng, Ting ‐ Jen R.; Chan, Ting ‐ Hao; Tsou, En ‐ Lun; Chang, Shang ‐ Yu; Yun, Wen ‐ Yi; Yang, Pei ‐ Jung; Wu, Ying ‐ Ta; Cheng, Wei ‐ Chieh
- Abstract
A little inspiration: The systematic preparation of sixteen natural product ‐ inspired polyhydroylated pyrrolidine ‐ based isomeric scaffolds is described. Each scaffold possesses four stereogenic centers and one exo ‐ aminomethyl moiety, which allows for rapid substituent diversity. To exemplify biological applications, these new privileged scaffolds were used to discover new human Golgi α ‐ mannosidase II inhibitors. The most potent inhibitor shows competitive behavior with a Ki value of 24 nM.
- Subjects
MANNOSIDASES; CHEMICAL inhibitors; PYRROLIDINE synthesis; HOMOLOGY (Biology)
- Publication
Chemistry - An Asian Journal, 2013, Vol 8, Issue 11, p2600
- ISSN
1861-4728
- Publication type
Article
- DOI
10.1002/asia.201300680