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.
Beevers
Rebekah E
RE
UCB Celltech, Granta Park, Great Abington, Cambridge, CB1 6GS, UK.
Buckley
George M
GM
Davies
Natasha
N
Fraser
Joanne L
JL
Galvin
Francis C
FC
Hannah
Duncan R
DR
Haughan
Alan F
AF
Jenkins
Kerry
K
Mack
Stephen R
SR
Pitt
William R
WR
Ratcliffe
Andrew J
AJ
Richard
Marianna D
MD
Sabin
Verity
V
Sharpe
Andrew
A
Williams
Sophie C
SC
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