13754-45-5Relevant articles and documents
Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms
Mancuso, Francesca,Di Fiore, Anna,De Luca, Laura,Angeli, Andrea,Monti, Simona M.,De Simone, Giuseppina,Supuran, Claudiu T.,Gitto, Rosaria
supporting information, p. 1000 - 1005 (2020/03/23)
We report the synthesis and biochemical evaluation of a series of substituted 4-(4-aroylpiperazine-1-carbonyl)benzenesulfonamides (5a-s) developed as inhibitors of druggable carbonic anhydrase (CA) isoforms, as tools for the identification of new therapeu
Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib
Pan, Xiaoyan,Dong, Jinyun,Shao, Ruili,Su, Ping,Shi, Yaling,Wang, Jinfeng,He, Langchong
supporting information, p. 4164 - 4168 (2015/11/03)
In order to expand the structural diversity of Bcr-Abl inhibitors, twenty hybrids (series E and P) have been synthesized and characterized based on Imatinib and GNF-2. Their biological activities were evaluated in vitro against human leukemia cells. Most compounds exhibited potent antiproliferative activity against K562 cells, especially for compounds E4, E5 and E7. Furthermore, these new hybrids were also screened for Abl kinase inhibitory activity, and some of them inhibited Abl kinase with low micromolar IC50 values. In particular, compound P3 displayed the most potent activity with IC50 value of 0.017 μM comparable with that of Imatinib. Molecular docking studies indicated that these novel hybrids fitted well with the active site of Bcr-Abl. These results suggested the great potential of these compounds as novel Bcr-Abl inhibitors.
Synthesis and evaluation of meta substituted 1-(aryloxypropyl)-4- (chloroaryl) piperazines as potential atypical antipsychotics
Bali, Alka,Reddy, A. C. Dinesh Kumar
, p. 382 - 391 (2013/03/13)
A series of 1-(aryloxypropyl)-4-(chloroaryl) piperazines have been synthesized based upon their physicochemical similarity with respect to standard atypical antipsychotic drugs and their potential to cross the blood-brain barrier (log BB) as calculated by