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 RAW 264.7 cell line in order to investigate their ability to modulate the production of Prostaglandin E 2 (PGE 2). This optimization process led to the identification of three strictly correlated compounds with comparable and higher inhibitory potency than BLQ on PGE 2 production. To evaluate the affinity of BLQ and its analogues for hsPLA 2, surface plasmon resonance (SPR) experiments were performed. © 2010 Elsevier Masson SAS. All rights reserved.
Structure-based design, synthesis and preliminary anti-inflammatory activity of bolinaquinone analogues
Filosa R.
;
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 RAW 264.7 cell line in order to investigate their ability to modulate the production of Prostaglandin E 2 (PGE 2). This optimization process led to the identification of three strictly correlated compounds with comparable and higher inhibitory potency than BLQ on PGE 2 production. To evaluate the affinity of BLQ and its analogues for hsPLA 2, surface plasmon resonance (SPR) experiments were performed. © 2010 Elsevier Masson SAS. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
