851769-54-5Relevant 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 anti-tumor activity of (2-O-alkyloxime-3-phenyl)- propionyl-1-O-acetylbritannilactone esters
Liu, Shouxin,Liu, He,Yan, Weiying,Zhang, Li,Bai, Naisheng,Ho, Chi-Tang
, p. 2783 - 2789 (2007/10/03)
The extracts of Inula britannica have anti-inflammatory, anti-bacterial, anti-hepatitic, and anti-tumor activities. Various sesquiterpene lactones with cytotoxic properties including 1-O-acetylbritannilactone (1) have been isolated from this Chinese medic
