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

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

  • Bioorg Med Chem Lett. 2010 May 15;20(10):3155-7. doi: 10.1016/j.bmcl.2010.03.087.
Yongchun Shen 1,  Roch Boivin,  Naoki Yoneda,  Hong Du,  Shawn Schiller,  Tomohiro Matsushima,  Masaki Goto,  Hiroshi Shirota,  Fabian Gusovsky,  Charles Lemelin,  Yimin Jiang,  Zhiyi Zhang,  Robert Pelletier,  Megumi Ikemori-Kawada,  Yoshiyuki Kawakami,  Atsushi Inoue,  Matthew Schnaderbeck,  Yuan Wang
Affiliations

Affiliation

  • 1 Eisai Inc., Andover, MA 01810, USA.
PMID: 20399648 DOI: 10.1016/j.bmcl.2010.03.087
Abstract

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.

Figures