Introduction

The present invention relates to new synthetic analogues of Xanthumol (XN), a prenylated chalcone of natural origin found in the female inflorescence of the hop plant (Humulus lupulus L.-Cannabaceae). The new compounds showed anti-angiogenic, antioxidant and chemopreventive properties and their anti-proliferative, anti-invasive, anti-angiogenic activity is greater than the natural compound.

Technical features

Xanthumol is a flavonoid known for its multiple properties: anti-invasive, antiproliferative, antiangiogenic, pro-apoptotic, antibacterial, inhibitory on cytochrome P450 enzymes involved in the metabolic activation of carcinogenesis and anti-inflammatory, exerted through the reduction of oxide production nitrate (NO). However, the therapeutic use of Xanthumol of natural origin presents some critical issues due to its low potency and selectivity. The new molecules with a structure similar to natural Xanthumol are more effective compounds in the treatment of degenerative processes characterized by phenomena of cellular hyperproliferation, angiogenesis, tissue destruction from uncontrolled hyperproteolysis and which can show better properties in terms of bioavailability, efficacy and reduced toxicity compared to known compound.

Possible Applications

• Prevention and treatment of diseases where hyperproliferative processes are involved;
• Treatment of tumors;
• Treatment of diseases in which inflammatory processes are involved;
• Treatment of cardiovascular and neurodegenerative diseases.

Advantages

• Higher activity and lower toxicity than the natural compound;
• Action on multiple molecular targets, useful to prevent the emergence of possible tumor resistance;
• Inhibition of angiogenesis, essential in the prevention and/or treatment of tumor angiogenesis.