Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity

Synthetic and computational efforts towards the development of peptidomimetics and small-molecule SARS-CoV 3CLpro inhibitors

“…A major class of heterocyclic compounds that exist in many drugs and synthetic products are pyrazolone derivatives 91 . Such molecules has excellent analgesic 91 , antituberculosis 93 , antifungal 92 , antimicrobial 93 , anti-inflammatory 94 , antioxidant 96 and anti-tumor functions 97 . The pyrazolone structure plays an important role because of its easy preparation and rich biological activity and represents a fascinating template for combinatorial and medicinal chemistry.…”

4-Disubstituted Pyrazolin-3-Ones—Novel Class of Fungicides against Phytopathogenic Fungi

“…The interest of medicinal chemists to pyrazolones has been maintained and is increasing at the present time [22]. Recently, C4-disubstituted pyrazolones, primarily spiropyrazolones, have also attracted increasing attention as biologically active compounds [34][35][36]. Due to the wide spectrum of the biological activity of disubstituted pyrazolones, new asymmetric methods for their synthesis are being actively developed [36][37][38][39][40][41].…”

“…Due to the wide spectrum of the biological activity of disubstituted pyrazolones, new asymmetric methods for their synthesis are being actively developed [36][37][38][39][40][41]. C4-disubstituted pyrazolones are recognized as valuable antitumor agents [35,[42][43][44][45][46], antimicrobial substances [47], inhibitors of trypanosomal phosphodiesterase B1 [48], RalA inhibitors [49], and miticides [50]. However, their potential as effective fungicides has not been expected.…”

4-Nitropyrazolin-5-ones as Readily Available Fungicides of the Novel Structural Type for Crop Protection: Atom-Efficient Scalable Synthesis and Key Structural Features Responsible for Activity

“…Pyrazolones are widely known as a class of heterocycles with a broad spectrum of biological activity. 31 Compounds containing a pyrazolone ring possess anti-inflammatory, 32 analgesic, 33 antibacterial, 34,35 hypoglycemic, 36 and antitumor 37,38 effects, among them are p38 MAP kinase inhibitors, 39 HIV-1 integrase inhibitors, 40 4-phosphodiesterase inhibitors, 41,42 and HNO donors. 43,44 ophenyl)-3-methyl-5-pyrazolone (TELIN) is considered as an active substance for treatment of cancer and related diseases.…”

“…Pyrazolones are widely known as a class of heterocycles with a broad spectrum of biological activity . Compounds containing a pyrazolone ring possess anti-inflammatory, analgesic, antibacterial, , hypoglycemic, and antitumor , effects, among them are p38 MAP kinase inhibitors, HIV-1 integrase inhibitors, 4-phosphodiesterase inhibitors, , and HNO donors. , 4,4-Dichloro-1-(2,4-dichlorophenyl)-3-methyl-5-pyrazolone (TELIN) is considered as an active substance for treatment of cancer and related diseases . Several compounds are also registered as drugs: the neuroprotector edaravone (1-phenyl-3-methyl-5-pyrazolone) is effective in acute ischemic stroke and amyotrophic lateral sclerosis, and phenazone derivatives are anti-inflammatory drugs used in many analgesic combinations. , A number of pyrazolones exhibit herbicidal − and fungicidal ,− properties; however, the activity is not associated with the presence of the pyrazolone ring itself, and such molecules contain other moieties essential for the manifested activity.…”