Synthesis and biological evaluation of β-chloro vinyl chalcones as inhibitors of TNF-α and IL-6 with antimicrobial activity

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

“…The same investigators [26] synthesized a series of β-chloro-vinyl chalcones and evaluated their ability to inhibit IL-6. The QSAR analysis ( The term σ p stands for the electronic effect of p-substituents (Hammett's constant).…”

“…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 and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents

“…Antimicrobial activities of all the synthesized compounds were determined by disc diffusion method 41 . All the bacterial and fungal species used were procured from Institute of Microbial Type Culture Collection (IMTCC), Chandigarh, India, and National Collection of Industrial Microorganisms (NCIM), Pune, India, namely, Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Shigella flexenari, Salmonella typhi, Candida albicans, and Aspergillus niger.…”

Synthesis and Molecular modeling of some new chalcones derived from coumarine as CDC25 phosphatases inhibitors

“…Wide range of different scaffolds has been reported as CDC25 phosphatase inhibitors including quinoids, dysidiolide and large collection of miscellaneous structures 6,7 . Chalcones have numerous biological activities containing antihypertensive, antifungal, anticonvulsant, antiviral, antioxidant, anti-inflammatory, antimalarial, anti-HIV, antiprotozoal, antimicrobial, antifilarial, 8,9 they also proved their antitumor activities through their action against many molecular targets 10 . The substituted chalcones in position 4 of ring (B) was even reported as CDC25 inhibitors with considerable activity (Figure 1) 11 .Coumarines are well known as anticancer 12 active compounds with many different mechanisms like kinase inhibitors, apoptosis induction, angiogenetic inhibition, HSP90 inhibitors, telomerase inhibitor and antimitotic.…”