477204-95-8Relevant academic research and scientific papers
Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors
Zhuang, Rangxiao,Gao, Lixin,Lv, Xiaoqing,Xi, Jianjun,Sheng, Li,Zhao, Yanmei,He, Ruoyu,Hu, Xiaobei,Shao, Yidan,Pan, Xuwang,Liu, Shourong,Huang, Weiwei,Zhou, Yubo,Li, Jia,Zhang, Jiankang
, p. 1056 - 1070 (2017/01/22)
A series of novel piperazine or piperidine-containing non-covalent peptidyl derivatives possessing a neopentyl-asparagine residue were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were screened for their 20S proteasom
Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold
Giannini, Giuseppe,Battistuzzi, Gianfranco,Vesci, Loredana,Milazzo, Ferdinando M.,De Paolis, Francesca,Barbarino, Marcella,Guglielmi, Mario Berardino,Carollo, Valeria,Gallo, Grazia,Artali, Roberto,Dallavalle, Sabrina
, p. 462 - 466 (2014/01/23)
Poly(ADP-ribose)polymerase-I (PARP-1) enzyme is involved in maintaining DNA integrity and programmed cell death. A virtual screening of commercial libraries led to the identification of five novel scaffolds with inhibitory profile in the low nanomolar range. A hit-to-lead optimization led to the identification of a group of new potent PARP-1 inhibitors, acyl- piperazinylamides of 3-(4-oxo-3,4-dihydro-quinazolin-2-yl)-propionic acid. Molecular modeling studies highlighted the preponderant role of the propanoyl side chain.
