Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases.
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.
Lazarova
Tsvetelina
T
Enanta Pharmaceuticals, 500 Arsenal Street, Watertown, Massachusetts 02472, USA. tsvetelina.lazarova@sprlus.com
Chen
Jason S
JS
Hamann
Blake
B
Kang
Jane M
JM
Homuth-Trombino
Daniela
D
Han
Feng
F
Hoffmann
Ethan
E
McClure
Christopher
C
Eckstein
Jens
J
Or
Yat Sun
YS
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
D065095:Calcineurin Inhibitors; D003524:Cyclosporins; D007166:Immunosuppressive Agents