Key result
Phe-Gly dipeptide-derived piperazinones fail to inhibit human platelet aggregation or demonstrate cytotoxicity in cancer cells.
Why the study?
New Phe-Gly dipeptide-derived piperazinones were synthesized to explore their potential as antagonists of the thrombin receptor PAR1 and inhibitors of platelet aggregation.
The synthesized Phe-Gly dipeptide-derived piperazinones failed to demonstrate activity as PAR1 antagonists or cytotoxic agents in vitro.
Null results in vitro do not support advancement; leaves open whether scaffold modifications merit further preclinical testing.
A series of Phe-Gly dipeptide-derived piperazinones containing an aromatic urea moiety and a basic amino acid has been synthesized and evaluated as inhibitors of human platelet aggregation induced by the PAR1 agonist SFLLRN and as cytotoxic agents in human cancer cells. The synthetic strategy involves coupling of a protected basic amino acid benzyl amide to 1,2- and 1,2,4-substituted-piperazinone derivatives, through a carbonylmethyl group at the N1-position, followed by formation of an aromatic urea at the exocyclic moiety linked at the C2 position of the piperazine ring and removal of protecting groups. None of the compounds showed activity in the biological evaluation.
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Valdivielso et al. (2014) studied this question. Phe-Gly dipeptide-derived piperazinones was evaluated on Inhibition of human platelet aggregation and cytotoxicity in human cancer cells. None of the synthesized Phe-Gly dipeptide-derived piperazinones showed activity as inhibitors of human platelet aggregation or as cytotoxic agents in human cancer cells.
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