49557-37-1Relevant academic research and scientific papers
Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines
Tian, Xia,Feng, Juan,Fan, Shi-ming,zhen, Xiao-li,Han, Jian-rong,Liu, Shou-xin
, p. 5197 - 5205 (2016/10/24)
A series of arylidene N-alkoxydiketopiperazines was designed and stereoselectively synthesized via oxime-ether formation and intramolecular acylation. Possible cyclization and acid-catalyzed rearrangement-fragmentation mechanisms were discussed. The crystal structure of the novel diketopiperazine further confirmed the rearrangement mechanism. Most compounds exhibited antitumor activity. Several compounds were more potent against caspase-3. Specifically, compounds 6e, 6g, and 6f inhibited caspase-3 at IC50values lying within the low micromolar range and demonstrated good selectivity. The binding modes of alkoxydiketopiperazines in the active center of caspase-3 were also discussed based on the molecular docking results.
Stereoselective synthesis and rearrangement-fragmentation of arylidene N-alkoxydiketopiperazines
Liu, Shouxin,Mu, Yun,Han, Jianrong,Zhen, Xiaoli,Yang, Yihua,Tian, Xia,Whiting, Andrew
experimental part, p. 7476 - 7481 (2011/12/03)
A stereoselective synthesis of arylidene N-alkoxydiketopiperazines via oxime-ether formation and intramolecular acylation is described, followed by an acid-catalysed rearrangement-fragmentation to give novel diketopiperazine hemiaminal derivatives with us
