title: Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases.
abstract: Cyclosporin A is effective in the treatment of asthma patients, but its chronic use is limited by toxicity. Novel cyclosporin A analogues were synthesized utilizing the olefin metathesis reaction and evaluated in a calcineurin A inhibition assay. The novel analogues demonstrated activity comparable to activity of the parent molecule and are potential soft drugs.
authors.affiliation: Enanta Pharmaceuticals, 500 Arsenal Street, Watertown, Massachusetts 02472, USA. tsvetelina.lazarova@sprlus.com
authors.forename: Tsvetelina
authors.initials: T
authors.lastname: Lazarova
authors.forename: Jason S
authors.initials: JS
authors.lastname: Chen
authors.forename: Blake
authors.initials: B
authors.lastname: Hamann
authors.forename: Jane M
authors.initials: JM
authors.lastname: Kang
authors.forename: Daniela
authors.initials: D
authors.lastname: Homuth-Trombino
authors.forename: Feng
authors.initials: F
authors.lastname: Han
authors.forename: Ethan
authors.initials: E
authors.lastname: Hoffmann
authors.forename: Christopher
authors.initials: C
authors.lastname: McClure
authors.forename: Jens
authors.initials: J
authors.lastname: Eckstein
authors.forename: Yat Sun
authors.initials: YS
authors.lastname: Or
mesh_terms: D001327:Autoimmune Diseases / Q000188:drug therapy; D065095:Calcineurin Inhibitors; D003524:Cyclosporins / Q000138:chemical synthesis* / Q000737:chemistry; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D065095:Calcineurin Inhibitors; D003524:Cyclosporins; D007166:Immunosuppressive Agents