68014-13-1

Upstream product

• 123-66-0 Ethyl hexanoate 
• 95-92-1 oxalic acid diethyl ester 
• 122-56-5 tributyl borane 
• 615-94-1 2,5-dihydroxy-1,4-benzoquinone 
• 67820-74-0 2,2,6,6-tetramethylbenzo[1,2-d;4,5-d¹]bis[1,3]dioxole 
• 636-32-8 1,2,4,5-benzenetetrol 
• 1609067-69-7 C₂₀H₃₀O₄ 

Relevant academic research and scientific papers

The benzoquinone derivatives and their use

The invention provides a p-benzoquinone derivative and an application thereof. The p-benzoquinone derivative has the inhibitory activity on a plasminogen activator inhibitor-1 (PAI-1); on cellular level, the compound can inhibit the transfer ability of HepG2 liver cancer cells; and in-vitro experiments show that the compound has an inhibition effect on formation of fibrin clots. The p-benzoquinone derivative can be used as a medicine for treating tumors and thrombotic diseases.

Design, synthesis, and SAR of embelin analogues as the inhibitors of PAI-1 (plasminogen activator inhibitor-1)

The natural product embelin was found to have PAI-1 inhibitory activity with the IC50 value of 4.94 μM. Based on the structure of embelin, a series of analogues were designed, synthesized, and evaluated for their ability to inhibit PAI-1. The SAR study on these compounds disclosed that the inhibitory potency largely depended on the hydroxyl groups at C2 and C5, and the length of the alkyl chains at C3 and C6. Compound 11 displayed the best PAI-1 inhibitory potency with the IC50 value of 0.18 μM.