title: The synthesis and selective IL-2 inhibitory activity of bis piperazine-phenol Mannich adducts.
abstract: 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.
authors.affiliation: ArQule, Inc., 19 Presidential Way, Woburn, MA 01801, USA. bgeng@arqule.com
authors.forename: Bolin
authors.initials: B
authors.lastname: Geng
authors.forename: Paul R
authors.initials: PR
authors.lastname: Fleming
authors.forename: Scott
authors.initials: S
authors.lastname: Umlauf
authors.forename: Augustine
authors.initials: A
authors.lastname: Lin
authors.forename: Peter V
authors.initials: PV
authors.lastname: Pallai
mesh_terms: 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
chemical_list: D000199:Actins; D018736:DNA Adducts; D007376:Interleukin-2; D008352:Mannich Bases; D010636:Phenols; D010879:Piperazines; D008156:Luciferases