2930-02-1Relevant articles and documents
Synthesis and evaluation of 4-(2-hydroxypropyl)piperazin-1-yl) derivatives as Hsp90 inhibitors
Cherfaoui, Bahidja,Guo, Tian-Kun,Sun, Hao-Peng,Cheng, Wei-Lin,Liu, Fang,Jiang, Fen,Xu, Xiao-Li,You, Qi-Dong
supporting information, p. 2423 - 2432 (2016/05/24)
We previously reported 4-(3-((6-bromonaphthalen-2-yl)oxy)-2-hydroxypropyl)-N,N-dimethylpiperazine-1-sulfonamide (1) as a novel heat shock protein 90 inhibitor with moderate activity. In our ongoing efforts for the discovery of Hsp90 modulators we undertake structural investigations on 1. Series of the titled compound were designed, synthesized and evaluated. We have found that compounds with a hydroxyl group at C-4 of the aryl ring on the piperazine moiety possess Hsp90 inhibition properties. Compound 6f with improved activity could be further developed and optimized as Hsp90 inhibitor.
Thienopyrimidines as β3-adrenoceptor agonists: Hit-to-lead optimization
Tasler, Stefan,Baumgartner, Roland,Ammendola, Astrid,Schachtner, Josef,Wieber, Tanja,Blisse, Marcus,Rath, Sandra,Zaja, Mirko,Klahn, Philipp,Quotschalla, Udo,Ney, Peter
scheme or table, p. 6108 - 6115 (2010/11/19)
Resulting from a vHTS based on a pharmacophore alignment on known β3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human β3-AR agonist, yielding a lead compound with an excellent cellular activity of EC50 = 20 pM, selectivity over hβ1- and hβ2-adrenoceptors and a promising safety profile.