22974-74-9Relevant articles and documents
Design, synthesis, and biological evaluation of conformationally constrained analogues of naphthol AS-E as inhibitors of CREB-mediated gene transcription
Jiang, Min,Li, Bingbing X.,Xie, Fuchun,Delaney, Frances,Xiao, Xiangshu
scheme or table, p. 4020 - 4024 (2012/07/16)
Cyclic AMP response element binding protein (CREB) is often dysregulated in cancer cells and is an attractive cancer drug target. Previously, we described naphthol AS-E (1) as a small molecule inhibitor of CREB-mediated gene transcription. To understand its bioactive conformation, a series of conformationally constrained analogues of 1 were designed and synthesized. Biological evaluation of these analogues suggests that the global energy minimum of 1 is the likely bioactive conformation.
Hydroxamic acid and pharmaceutical preparations containing the same
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, (2008/06/13)
Hydroxamic acids, pharmaceutical preparations containing the same, new ω(2''-naphthoxy)-alkylhydroxamic acids as well as a process for their production are disclosed. The new compounds display antiasthmatic and further pharmacologically valuable characteristics. They are prepared by reacting the corresponding carboxylic acid ester or amide with hydroxylamine or its salt under the described conditions into compounds of Formula I,R--CO--NH--OH.The compounds of Formula I are useful in human and veterinary medicine as medicaments the active principal of which is the inhibition of lipoxygenase, thus as antiasthmatic, antianaphylactic, antiphlogistic, antirheumatic and antithrombotic preparations.