Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
The development of a series of novel quinazolinethiones and quinazolinediones as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II and in vitro inhibitory value for PBMC proliferation are discussed.
Buckley
George M
GM
Celltech R and D, Granta Park, Great Abington, Cambridge CB1 6GS, UK.
Davies
Natasha
N
Dyke
Hazel J
HJ
Gilbert
Philip J
PJ
Hannah
Duncan R
DR
Haughan
Alan F
AF
Hunt
Caroline A
CA
Pitt
William R
WR
Profit
Rachael H
RH
Ray
Nicholas C
NC
Richard
Marianna D
MD
Sharpe
Andrew
A
Taylor
Alicia J
AJ
Whitworth
Justine M
JM
Williams
Sophie C
SC
D001773:Blood Cells; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000138:chemical synthesis / Q000494:pharmacology; D009000:Monocytes / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013871:Thiones / Q000138:chemical synthesis / Q000494:pharmacology
D004791:Enzyme Inhibitors; D007659:Ketones; D011799:Quinazolines; D013871:Thiones; D007168:IMP Dehydrogenase; C488211:IMPDH1 protein, human