40808-21-7Relevant articles and documents
Hedgehog signal pathway inhibitor
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Paragraph 0103; 0181, (2017/06/20)
The invention provides a Hedgehog signal pathway inhibitor as well as stereoisomers, tautomers, hydrates, solvates or pharmaceutically acceptable salts thereof, and the structural formula of the inhibitor is as shown in a formula (I). The invention further provides a preparation method and application of a compound. The compound provided by the invention is novel in structure; a signal transduction pathway adjusted by Hedgehog protein, Ptch, Gli and/or Smo can be adjusted through the compound of the formula I.
Synthesis and structure-activity relationships of 5-phenylthiophenecarboxylic acid derivatives as antirheumatic agents
Noguchi, Toshiya,Hasegawa, Masahiro,Tomisawa, Kazuyuki,Mitsukuchi, Morihiro
, p. 4729 - 4742 (2007/10/03)
5-(Phenylthiophene)-3-carboxylic acid (2a), a metabolite of esonarimod (1), which was developed as a new antirheumatic drug, was considered as a lead compound for new antirheumatic drugs. A new series of 2a derivatives were synthesized and their characteristic pharmacological effects, that is their antagonistic effect toward interleukin (IL)-1 in mice and the suppressive effect against adjuvant-induced arthritis (AIA) in rats, were evaluated and compared with those of 1. The structure-activity relationships indicated that [5-(4-bromophenyl)-thiophen-3-yl]acetic acid (5d), methyl [5-(4-chlorophenyl)-thiophen-3-yl]acetate (5h), and methyl [5-(4-bromophenyl)-thiophen-3-yl]acetate (5i) suppressed AIA more potently than 1 and all of the other synthesized compounds.