1345343-86-3Relevant 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.
Design, synthesis, and antitumor activity of novel acylate of 6-OH at 1- O-acetylbritannilactone
Liu, Shouxin,Feng, Jun,Liu, He,Li, Junzhang,Tian, Xia
, p. 200 - 205 (2015/04/14)
N-(α-Alkyloxime-3-phenylpropionyl) proline was designed and synthesized as an acylating agent to modify the 6-OH of 1-O-acetylbritannilactone. Eight intermediates and eight target compounds were obtained. The structures of sixteen novel compounds were characterized by 1HNMR, IR and HRMS. The activities against HL-60 and Bel-7402 cell lines were tested, the IC50 values of compound IVg were 2.7 μM and 4.3 μM, respectively.
Stereoselective synthesis and rearrangement-fragmentation of arylidene N-alkoxydiketopiperazines
Liu, Shouxin,Mu, Yun,Han, Jianrong,Zhen, Xiaoli,Yang, Yihua,Tian, Xia,Whiting, Andrew
, 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
