title: C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study.
abstract: A tether length study of C32-O-phenalkyl ether derivatives of ascomycin was conducted wherein it was determined that a 2-carbon tether provides optimum in vitro immunosuppressive activity. Oxygen-bearing substituents along the 2-carbon tether can further increase the potency of this design.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: M T
authors.initials: MT
authors.lastname: Goulet
authors.forename: P J
authors.initials: PJ
authors.lastname: Sinclair
authors.forename: F
authors.initials: F
authors.lastname: Wong
authors.forename: M J
authors.initials: MJ
authors.lastname: Staruch
authors.forename: F J
authors.initials: FJ
authors.lastname: Dumont
authors.forename: J G
authors.initials: JG
authors.lastname: Cryan
authors.forename: G J
authors.initials: GJ
authors.lastname: Wiederrecht
authors.forename: M J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: W H
authors.initials: WH
authors.lastname: Parsons
mesh_terms: D000818:Animals; D002455:Cell Division / Q000187:drug effects; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D020104:Immunophilins / Q000378:metabolism; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D018942:Macrolides / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects; D016559:Tacrolimus / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D022021:Tacrolimus Binding Proteins
chemical_list: D007166:Immunosuppressive Agents; D018942:Macrolides; C058028:immunomycin; D022021:Tacrolimus Binding Proteins; D020104:Immunophilins; D016559:Tacrolimus