1-Acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles: Exhibiting anticancer activity through intracellular ROS scavenging and the mitochondria-dependent death pathway
Alex, Jimi M.
MetadataShow full item record
A series of 17 analogs of 1-acetyl-4,5-dihydro(1H)pyrazoles (JP-1 to JP-17) bearing two aromatic rings at positions 3 and 5, either of which ought to be heterocyclic, were synthesized and evaluated for their anti-proliferative potential against breast cancer (MCF-7 and T-47D) and lung cancer (H-460 and A-549) cell lines for the first time. JP-1-7, -10, -11, -14, and -15 were observed to exhibit significant anti-proliferative activity against MCF-7 cells. Some notions about structure-activity relationships are reported. The investigated compounds were found to lower the intracellular reactive oxygen species in the H2DCFDA assay and also caused mitochondria-dependent cell death in the MCF-7 cell line, indicating a plausible mechanism of their anticancer effect. Analogs of 1-acetyl-4,5-dihydro(1H)pyrazoles (JP-1-17) were synthesized and evaluated for their anti-proliferative activity in four cancer cell lines and for their intracellular ROS scavenging properties. An attempt was made to determine the mitochondrial membrane potential of MCF-7 cells treated with JP-1 and -14, aiming to elucidate the mechanism by which proliferation was curbed. ? 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Archiv der Pharmazie
Showing items related by title, author, creator and subject.
4,5-Dihydro-1H-pyrazole: An indispensable scaffold Alex, Jimi Marin; Kumar, Raj (Informa Healthcare, 2014)Pyrazoles, categorized as nitrogen-containing heterocycles, are well known for their interminable participation in the field of perpetual research and development of therapeutical active agents. As a consequence pyrazoles ...
Synthesis, Characterization and Biological Evaluation of 5-(2- Nitrophenyl)-1H-Pyrazole Derivatives as Putative Antiproliferative Agents Saini, Geetika (Central University of Punjab, 2018)Pyrazoles are known to exhibit various biological activities like antibacterial, antiprotozoal, anticonvulsant, analgesic, anti-inflammatory, antiviral and antiproliferative. An attempt has been made to synthesize substituted ...
Pyrimidine-fused derivatives: Synthetic strategies and medicinal attributes Joshi, Gaurav; Nayyar, Himanshu; Alex, Jimi Marin; Vishwakarma, Gajendra S.; Mittal, Sunil; Kumar, Raj (Bentham Science Publishers B.V., 2016)Pyrimidine-fused derivatives traits the inextricable part of DNA and RNA, exhibit indispensable role in numerous biological processes, possessing momentous chemical and biological importance. Pyrimidine-condensed derivatives ...