Novel indole inhibitors of IMPDH from fragments: synthesis and initial structure-activity relationships.
The elaboration of previously reported indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II, PBMC proliferation and physicochemical properties are discussed.
UCB Celltech, Granta Park, Great Abington, Cambridge, CB1 6GS, UK.
Rebekah E
RE
Beevers
George M
GM
Buckley
Natasha
N
Davies
Joanne L
JL
Fraser
Francis C
FC
Galvin
Duncan R
DR
Hannah
Alan F
AF
Haughan
Kerry
K
Jenkins
Stephen R
SR
Mack
William R
WR
Pitt
Andrew J
AJ
Ratcliffe
Marianna D
MD
Richard
Verity
V
Sabin
Andrew
A
Sharpe
Sophie C
SC
Williams
D001693:Biological Transport, Active / Q000187:drug effects; D018938:Caco-2 Cells; D049109:Cell Proliferation / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D015394:Molecular Structure; D008970:Molecular Weight; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D007211:Indoles; D007168:IMP Dehydrogenase