105686-93-9Relevant academic research and scientific papers
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation, and ulcerogenic liability of new 1,3,5-triarylpyrazoline derivatives possessing a methanesulfonyl pharmacophore
Abdellatif, Khaled R. A.,Fadaly, Wael A. A.,Azouz, Amany A.
, p. 1 - 7 (2016)
A new series of 1,3,5-triarylpyrazolines 13a–l was synthesized and all prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and in vivo anti-inflammatory activity. All test compounds were more selective for the COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 13h was the most COX-2 selective compound (COX-2 selectivity index (SI)=10.23) and the most potent anti-inflammatory derivative (ED50-60.1μmol/kg) in comparison with celecoxib (COX-2 SI=9.29 and ED50=81.4μmol/kg). All screened compounds were less ulcerogenic (ulcer indexes (UI)=0.33–1.33) than aspirin (UI=2.33) and comparable to celecoxib (UI=0.33).
Synthesis and biological evaluation of naphthalene, furan and pyrrole based chalcones as cytotoxic and antimicrobial agents
Budhiraja, Abhishek,Kadian, Kanika,Kaur, Mandeep,Aggarwal, Vikas,Garg, Atul,Sapra, Sameer,Nepali, Kunal,Suri,Dhar
, p. 2133 - 2140 (2012/11/07)
Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are collectively known as chalcones. These show antibacterial, antifungal, antitumour and antiinflammatory properties, and also are intermediates in the biosynthesis of flavonoids, substances widespread in plants with an array of biological activities. These biaryl propenones show potent toxicity to several cancer cell lines and interact with tubulin at its colchicine-binding site. Tubulin binding molecules interfere with the dynamic instability of microtubules and thereby disrupt microtubule inducing cell cycle arrest in the M phase, forming abnormal spindles and finally leading to apoptotic cell death. Basically Chalcones consists of C6-C3-C6 units but in the present study we report the reactions of 1-acetylnaphthalene, 2-acetylfuran and 2-acetylpyrrole with aldehydes, thus getting compounds akin to chalcones. 31 analogues have been synthesised and evaluated for cytotoxic potential against PC-3, OVCAR, IMR-32 and HEP-2. Compound 9 was found to be the most cytotoxic with inhibition ranging from 72 to 88% against the cell lines employed. The synthetics were also evaluated for antimicrobial activity and compound 25 was found to be the most potent. Springer Science+Business Media, LLC 2011.
Effect of ring A and ring B substitution on the cytotoxic potential of pyrazole tethered chalcones
Nepali, Kunal,Kadian, Kanika,Ojha, Ritu,Dhiman, Rajni,Garg, Atul,Singh, Gagandip,Buddhiraja, Abhishek,Bedi, Preet Mohinder Singh,Dhar, Kanaya Lal
, p. 2990 - 2997 (2012/10/29)
Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are collectively known as chalcones. The cytotoxic potential of chalcones which consists of C6-C 3-C6 units gets enhanced by the incorporation of pyrazole ring as proved by our earlier studies. Thus in the present work, pyrazoles of chalcones with ring A substituted by furan, naphthalene and variety of substituted phenyl rings has been prepared and evaluated for in vitro cytotoxic activity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines. Springer Science+Business Media, LLC 2011.
A rational approach for the design and synthesis of 1-acetyl-3,5-diaryl-4, 5-dihydro(1H)pyrazoles as a new class of potential non-purine xanthine oxidase inhibitors
Nepali, Kunal,Singh, Gurinderdeep,Turan, Anil,Agarwal, Amit,Sapra, Sameer,Kumar, Raj,Banerjee, Uttam C.,Verma, Prabhakar K.,Satti, Naresh K.,Gupta, Manish K.,Suri, Om P.,Dhar
experimental part, p. 1950 - 1958 (2011/04/27)
Xanthine oxidase is a complex molybdoflavoprotein that catalyses the hydroxylation of xanthine to uric acid. Fifty three analogues of 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles were rationally designed and synthesized and evaluated for in vitro xanthine
Studies on Cycloimmonium Ylids: Synthesis of Some New 2,4,6-Triarylsubstituted Pyridines via Pyridinium Ylids
Singhal, R. K.,Mishra, Naresh K.
, p. 1079 - 1080 (2007/10/02)
2,4,6-Triarylsubstituted pyridines (4a-r) have been synthesised by the reaction of pyridinium ylids (1a-c) with α,β-unsaturated ketones (2a-f) in the presence of ammonium acetate and acetic acid.These compounds (4a-r) have been characterised on the basis
