Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III

Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 ( 22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (10), p.3155-3157
Main Authors: Shen, Yongchun, Boivin, Roch, Yoneda, Naoki, Du, Hong, Schiller, Shawn, Matsushima, Tomohiro, Goto, Masaki, Shirota, Hiroshi, Gusovsky, Fabian, Lemelin, Charles, Jiang, Yimin, Zhang, Zhiyi, Pelletier, Robert, Ikemori-Kawada, Megumi, Kawakami, Yoshiyuki, Inoue, Atsushi, Schnaderbeck, Matthew, Wang, Yuan
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Anti-inflammatory
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - chemistry
Anti-Inflammatory Agents - pharmacokinetics
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Drug Discovery
f152A1
Lactones - chemical synthesis
Lactones - chemistry
Lactones - pharmacokinetics
LL-Z1640-2
Medical sciences
Mice
Pharmacology. Drug treatments
Resorcylic lactone
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 ( 22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.03.087