The synthesis and selective IL-2 inhibitory activity of bis piperazine-phenol Mannich adducts.
Novel phenol bis-Mannich adducts were identified as IL-2 expression inhibitors in a T cell proliferation screening assay. Analogues of the lead compound were prepared through parallel synthesis and a highly selective IL-2 inhibitor was discovered that provided a suitable compound for further optimization.
Geng
Bolin
B
ArQule, Inc., 19 Presidential Way, Woburn, MA 01801, USA. bgeng@arqule.com
Fleming
Paul R
PR
Umlauf
Scott
S
Lin
Augustine
A
Pallai
Peter V
PV
D000199:Actins / Q000235:genetics / Q000378:metabolism; D018736:DNA Adducts / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D007376:Interleukin-2 / Q000037:antagonists & inhibitors*; D019169:Jurkat Cells / Q000187:drug effects; D008156:Luciferases / Q000378:metabolism; D008352:Mannich Bases / Q000737:chemistry*; D010636:Phenols / Q000737:chemistry*; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011401:Promoter Regions, Genetic
D000199:Actins; D018736:DNA Adducts; D007376:Interleukin-2; D008352:Mannich Bases; D010636:Phenols; D010879:Piperazines; D008156:Luciferases