As a part of our drug discovery efforts we developed a series of simplified derivatives of bolinaquinone (BLQ), a hydroxyquinone marine metabolite, showing potent anti-inflammatory activity. Thirteen new hydroxyquinone derivatives closely related to BLQ were synthesized and tested on mouse macrophage-like RAW264.7 cell line in order to investigate their ability to modulate the production of Prostaglandin E2 (PGE2). This optimization process led to the identification of three strictly correlated compounds with comparable and higher inhibitory potency than BLQ on PGE2 production. To evaluate the affinity of BLQ and its analogues for hsPLA2, surface plasmon resonance (SPR) experiments were performed.

Structure-Based Design, Synthesis and Preliminary Anti-inflammatory Activity of Bolinaquinone Analogues

PETRONZI, CARMEN;PEDUTO, ANTONELLA;MONTI, Maria Chiara;MARGARUCCI, LUIGI;MASSA, Antonio;ERCOLINO, Simona Francesca;BIZZARRO, VALENTINA;PARENTE, Luca;RICCIO, Raffaele;DE CAPRARIIS, Paolo
2011-01-01

Abstract

As a part of our drug discovery efforts we developed a series of simplified derivatives of bolinaquinone (BLQ), a hydroxyquinone marine metabolite, showing potent anti-inflammatory activity. Thirteen new hydroxyquinone derivatives closely related to BLQ were synthesized and tested on mouse macrophage-like RAW264.7 cell line in order to investigate their ability to modulate the production of Prostaglandin E2 (PGE2). This optimization process led to the identification of three strictly correlated compounds with comparable and higher inhibitory potency than BLQ on PGE2 production. To evaluate the affinity of BLQ and its analogues for hsPLA2, surface plasmon resonance (SPR) experiments were performed.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11386/3036045
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