title: Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
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.
authors.affiliation: Eisai Inc., Andover, MA 01810, USA.
authors.forename: Yongchun
authors.initials: Y
authors.lastname: Shen
authors.forename: Roch
authors.initials: R
authors.lastname: Boivin
authors.forename: Naoki
authors.initials: N
authors.lastname: Yoneda
authors.forename: Hong
authors.initials: H
authors.lastname: Du
authors.forename: Shawn
authors.initials: S
authors.lastname: Schiller
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Matsushima
authors.forename: Masaki
authors.initials: M
authors.lastname: Goto
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Shirota
authors.forename: Fabian
authors.initials: F
authors.lastname: Gusovsky
authors.forename: Charles
authors.initials: C
authors.lastname: Lemelin
authors.forename: Yimin
authors.initials: Y
authors.lastname: Jiang
authors.forename: Zhiyi
authors.initials: Z
authors.lastname: Zhang
authors.forename: Robert
authors.initials: R
authors.lastname: Pelletier
authors.forename: Megumi
authors.initials: M
authors.lastname: Ikemori-Kawada
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Kawakami
authors.forename: Atsushi
authors.initials: A
authors.lastname: Inoue
authors.forename: Matthew
authors.initials: M
authors.lastname: Schnaderbeck
authors.forename: Yuan
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D055808:Drug Discovery; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051379:Mice; D013329:Structure-Activity Relationship
chemical_list: C545120:14-(ethylamino)-8,9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione; D000893:Anti-Inflammatory Agents; C118715:LL Z1640-2; D007783:Lactones