title: Structure and activity relationships of tartrate-based TACE inhibitors.
abstract: The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokinetics.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, 320 Bent Street, Cambridge, MA 02141, United States. dansu.li@spcorp.com
authors.forename: Dansu
authors.initials: D
authors.lastname: Li
authors.forename: Janeta
authors.initials: J
authors.lastname: Popovici-Muller
authors.forename: David B
authors.initials: DB
authors.lastname: Belanger
authors.forename: John
authors.initials: J
authors.lastname: Caldwell
authors.forename: Chaoyang
authors.initials: C
authors.lastname: Dai
authors.forename: Maria
authors.initials: M
authors.lastname: David
authors.forename: Vinay M
authors.initials: VM
authors.lastname: Girijavallabhan
authors.forename: Brian J
authors.initials: BJ
authors.lastname: Lavey
authors.forename: Joe F
authors.initials: JF
authors.lastname: Lee
authors.forename: Zhidan
authors.initials: Z
authors.lastname: Liu
authors.forename: Rob
authors.initials: R
authors.lastname: Mazzola
authors.forename: Razia
authors.initials: R
authors.lastname: Rizvi
authors.forename: Kristin E
authors.initials: KE
authors.lastname: Rosner
authors.forename: Bandarpalle
authors.initials: B
authors.lastname: Shankar
authors.forename: Jim
authors.initials: J
authors.lastname: Spitler
authors.forename: Pauline C
authors.initials: PC
authors.lastname: Ting
authors.forename: Henry
authors.initials: H
authors.lastname: Vaccaro
authors.forename: Wensheng
authors.initials: W
authors.lastname: Yu
authors.forename: Guowei
authors.initials: G
authors.lastname: Zhou
authors.forename: Zhaoning
authors.initials: Z
authors.lastname: Zhu
authors.forename: Xiaoda
authors.initials: X
authors.lastname: Niu
authors.forename: Jing
authors.initials: J
authors.lastname: Sun
authors.forename: Zhuyan
authors.initials: Z
authors.lastname: Guo
authors.forename: Peter
authors.initials: P
authors.lastname: Orth
authors.forename: Shiying
authors.initials: S
authors.lastname: Chen
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Kozlowski
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Lundell
authors.forename: Vincent
authors.initials: V
authors.lastname: Madison
authors.forename: Brian
authors.initials: B
authors.lastname: McKittrick
authors.forename: John J
authors.initials: JJ
authors.lastname: Piwinski
authors.forename: Neng-Yang
authors.initials: NY
authors.lastname: Shih
authors.forename: Gerald W
authors.initials: GW
authors.lastname: Shipps
authors.forename: M Arshad
authors.initials: MA
authors.lastname: Siddiqui
authors.forename: Corey O
authors.initials: CO
authors.lastname: Strickland
mesh_terms: D051722:ADAM Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000072198:ADAM17 Protein; D000818:Animals; D001665:Binding Sites; D003198:Computer Simulation; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013329:Structure-Activity Relationship; D013644:Tartrates / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D011480:Protease Inhibitors; D013644:Tartrates; D051722:ADAM Proteins; D000072198:ADAM17 Protein; C000606464:Adam17 protein, rat