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  • Title: Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines.
    Author: Tian X, Feng J, Fan SM, Zhen XL, Han JR, Liu SX.
    Journal: Bioorg Med Chem; 2016 Nov 01; 24(21):5197-5205. PubMed ID: 27594550.
    Abstract:
    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 IC50 values 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.
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