The chromones: history, chemistry and clinical development. A tribute to the work of Dr R. E. C. Altounyan

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

“…Several chromone derivatives have been reported for their clinical use as therapeutic agents. For example, khellin ( Figure 6), a natural product extracted from the seeds of the plant Ammi visnaga, was the first chromone-based therapy mainly used for centuries in the Mediterranean medicine as a diuretic, relaxant and also in the treatment of angina, asthma and vitiligo, a melanoma-driven pigmentation [92][93][94]. Daflon ® (diosmin) is a venotropic drug used in the treatment of venous diseases and hemorrhoids, while Lomudal ® (sodium cromoglycate) is clinically used for the treatment of asthma and allergies ( Figure 6) [95,96].…”

“…It also found in fruits (e.g., bilberry, cloudberry), green tea and other foods such as chicory. Coumarin derivatives possess a remarkable range of biological properties including antioxidant [109,110], vasorelaxant [111], antiviral (92,93) [112,113], anti-cancer (94,95), and anti-inflammatory activities [114,115]. Lastly, suksdorfin (96), another natural compound isolated from the fruit of Lomatium suksdorfii, exhibits a significant anti-HIV activity as it inhibits the viral replication in the T-cell line with an EC50 in the 2.5 µM range [116] (Figure 8).…”

Protective Therapy with Novel Chromone Derivative against <i>Leishmania donovani</i> Infection Induces Th1 Response in vivo

“…Chromones and their structural analogues are of great interest because of their usefulness as biologically active agents [1,2]. One of the first chromone analogues was produced based on khellin and was designated K18.…”

“…One of the first chromone analogues was produced based on khellin and was designated K18. Philip Sheard, from Bengers Pharmacology Department, revealed (unpublished experiments in 1954) that K18 could prevent bronchoconstriction [1]. Chromone derivatives, which are easily absorbed and metabolized, have been reported to display significant activities [1,2]: antimicrobial and antifungal, anti-inflammatory, immunostimulatory, HIV-inhibitory, antimutagenic, antiproliferative, inductive of cell cycle arrest and apoptosis, angiogenesis inhibition, even reversal of multidrug resistance.…”

“…Chromone derivatives, which are easily absorbed and metabolized, have been reported to display significant activities [1,2]: antimicrobial and antifungal, anti-inflammatory, immunostimulatory, HIV-inhibitory, antimutagenic, antiproliferative, inductive of cell cycle arrest and apoptosis, angiogenesis inhibition, even reversal of multidrug resistance. They were also found to act neuroprotectively and antipsychotically and exhibited antiplatelet aggregation effects [1,2]. …”