346629-82-1Relevant academic research and scientific papers
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: Structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor
Macdonald, Dwight,Mastracchio, Anthony,Perrier, Helene,Dube, Daniel,Gallant, Michel,Lacombe, Patrick,Deschenes, Denis,Roy, Bruno,Scheigetz, John,Bateman, Kevin,Li, Chun,Trimble, Laird A.,Day, Stephen,Chauret, Nathalie,Nicoll-Griffith, Deborah A.,Silva, Jose M.,Huang, Zheng,Laliberte, France,Liu, Susana,Ethier, Diane,Pon, Doug,Muise, Eric,Boulet, Louise,Chi, Chung Chan,Styhler, Angela,Charleson, Stella,Mancini, Joseph,Masson, Paul,Claveau, David,Nicholson, Donald,Turner, Mervyn,Young, Robert N.,Girard, Yves
, p. 5241 - 5246 (2005)
The discovery and SAR of a new series of substituted 8-arylquinoline PDE4 inhibitors are herein described. This work has led to the identification of several compounds with excellent in vitro and in vivo profiles, including a good therapeutic window of em
2,3-Diarylpropenoic acids as selective non-steroidal inhibitors of type-5 17β-hydroxysteroid dehydrogenase (AKR1C3)
Gazvoda, Martin,Beranic, Natasa,Turk, Samo,Burja, Bojan,Kocevar, Marijan,Rizner, Tea Lanisnik,Gobec, Stanislav,Polanc, Slovenko
supporting information, p. 89 - 97 (2013/05/09)
The aldo-keto reductase AKR1C3 is an important target for the development of new drugs. Selective inhibitors of this enzyme are needed because they should not inhibit other, structurally closely related AKR1C isoforms. A comprehensive series of 2,3-diarylpropenoic acids was synthesized and evaluated for the inhibition of AKR1C1-AKR1C3. We found that the 4-methylsulfonylphenyl substituent at position 2 of these acids is required to exhibit the selective inhibition of AKR1C3. The best results were obtained for the compounds that fulfill the above requirement and possess a 4-bromophenyl, 4-methylthiophenyl, 4-methylphenyl or 4-ethylphenyl substituent at position 3 of the substituted propenoic acids (i.e., acids 28, 29, 37, and 39, respectively). These compounds represent an important step toward the development of drug candidates for a treatment of the hormone-dependent and hormone-independent forms of prostate and breast cancers.
