Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-α and IL-6 inhibitors

Studies of synthetic chalcone derivatives as potential inhibitors of secretory phospholipase A2, cyclooxygenases, lipoxygenase and pro-inflammatory cytokines

“…The effect of α, β-unsaturated carbonyl based compounds on LOX enzyme was investigated by a standard colorimetric assay 33. Soybean LOX served as enzyme source.…”

“…Previous reports have also demonstrated the anti-inflammatory activity of chalcone derivatives by the modulation of pro-inflammatory gene expression of COX-2, inducible nitric oxide synthase, and numerous essential cytokines 29–32. Recent reports indicate the importance of chalcones as anti-inflammatory agents involved in inhibition of cell migration and inhibition of TNF-α production in a mouse model 33. Chalcones are also excellent skeletons for modification of drug design and development.…”

“…Chalcones are also excellent skeletons for modification of drug design and development. Recent findings by different groups of researchers suggested that some chalcones, such as the promising anti-inflammatory agents, exhibited their potential in the therapy of inflammatory and immune diseases 33–35. Chalcone derivatives have been extensively reported to inhibit NO synthesis and inducible NO synthetase and COX-2 protein expression in lipopolysaccharide (LPS) stimulated cells 34,36.…”

Cytokines in terms of QSAR. Review, evaluation and comparative studies

“…As IL-6 participates in various cellular and physiological responses during the inflammatory reaction [21], IL-6 inhibitors can be used in treatment of psychiatric disorders, Alzheimer's disease, diabetes, cancer, depression SAR and QSAR in Environmental Research 885 and rheumatoid arthritis [22][23][24]. Small compounds that are identified as IL-6 inhibitors (Figure 2) include nitrogen-containing benzophenones [25], β-chloro-vinyl chalcones [26,27], 4-styryl-coumarin derivatives [28], derivatives of N-aryl urea [29], methoxylated chalcones [30], thalidomide analogues [31], pyrazolo [3,4-b]pyridines [32], 3,5-diaryl pyridines and meta-terphenyls [33], 2,2-bisaminomethylated aurone analogues [34], pyrazole chalcones [35] and pyridine-5(6H)-one analogues [36]. Tocilizumab, an anti-interleukin-6 receptor antibody, has been approved for the treatment of rheumatoid arthritis, Castleman's disease and juvenile idiopathic arthritis [37].…”

Synthesis of novel 3,5-diaryl pyrazole derivatives using combinatorial chemistry as inhibitors of tyrosinase as well as potent anticancer, anti-inflammatory agents

“…6,7 Therefore, inhibition of these targets has become a major focus of current drug discovery and development, and an important in vitro method for evaluating the bioactivity of drugs. 8,9 Tyrosinase (EC 1.14.18.1), which is also referred to as polyphenoloxidase (PPO), is most widely associated with the production of melanin for the protection of skin from solar radiation. However, this beneficial trait comes in hand with some severe vices and human maladies since the overproduction of melanin results in skin hypigmentation, characterized by age spots, melasma and chloasama.…”