62353-80-4Relevant academic research and scientific papers
Synthesis and structure activity relationship studies of benzothieno[3,2-b]furan derivatives as a novel class of IKKβ inhibitors
Sugiyama, Hideyuki,Yoshida, Masato,Mori, Kouji,Kawamoto, Tomohiro,Sogabe, Satoshi,Takagi, Terufumi,Oki, Hideyuki,Tanaka, Toshimasa,Kimura, Hiroyuki,Ikeura, Yoshinori
, p. 613 - 624 (2008/02/13)
As a novel class of IKKβ inhibitors, a series of tricyclic furan derivatives was designed and synthesized based on the structure of known thiophene IKKβ inhibitors. Among the various fused furan derivatives synthesized, a benzothieno[3,2-b]furan derivative 13a displayed potent inhibitory activity towards IKKβ in enzymatic and cellular assays. The potent inhibitory activity originates from an intramolecular non-bonded S...O interaction which was confirmed by the X-ray structure of JNK3 with 16k. The introduction of further substituents on the core structure led to the discovery of the 6-alkoxy derivatives, which possessed a comparable IKKβ inhibitory activity to 13a and an improved metabolic stability. Among these, appropriately lipophilic compounds 16a, h, i, and 13g (logD>2) were found to possess good oral bioavailability.
Photochromatic substances
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, (2008/06/13)
Disclosed are adamantaneospiroheteroaromaticpyrans and adamantanospiro (1.3)oxazines of the general formula STR1 whereby R0 is a substituent from the series H, halogen, O-alkyl, N-alkyl, R1 -R4 : is a substituent from the series H, alkyl, aryl, subst. phenyl, naphthyl, heteroaryl, OH, alkoxy (C1 -C4), halogen, alkylamino, dialkylamino, cyan and trifluormethyl, or R1 and R2 or R3 and R4 or R2 and R3 are constituents of a condensed aromatic or heteroaromatic ring or an alkane ring with 4-8 C-atoms.
