1273924-72-3Relevant academic research and scientific papers
Synthesis and biological evaluation of novel pyrazolic chalcone derivatives as novel hepatocellular carcinoma therapeutics
Hawash, Mohammed M.A.,Kahraman, Deniz Cansen,Eren, Fikriye,Cetin Atalay, Rengul,Baytas, Sultan Nacak
, p. 12 - 26 (2017)
Despite having the second highest mortality associated with cancer, currently Sorafenib is the only FDA-approved chemotherapeutic agent available for liver cancer patients which can only improve survival for few months. In this study, various pyrazolic ch
Novel pyrazole-clubbed thiophene derivatives via Gewald synthesis as antibacterial and anti-inflammatory agents
Nayak, Soukhyarani G.,Poojary, Boja,Kamat, Vinuta
, (2020/09/09)
The aim of this study was to synthesize newer potent Schiff bases by condensing 2-amino-5-(2,4-dichlorophenyl)thiophene-3-carbonitrile and 1,3-disubstituted-1H-pyrazole-4-carbaldehydes, and to investigate their biological activity. The compounds were synthesized via Gewald synthesis and characterized by spectral data and elemental analyses. They were screened for their in vitro antibacterial and anti-inflammatory activities. The synthesized compounds were also evaluated for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Compounds 8b, 8c, 8f, 8g, 8k, 8n, and 8o showed promising antibacterial activity. The interactions between the substituted pyrazoles and bovine protein showed promising anti-inflammatory activity. The experimental results revealed compound 8a as a promising antitubercular agent. Hemolytic assays confirmed that the compounds are nontoxic, with percentage hemolysis ranging from 3.6 to 20.1, at a concentration of 1 mg/ml. The results suggest that the pyrazole ring and the substitution pattern on the heterocyclic moiety have an effect on the bioactivity.
Synthesis of ester and amide derivatives of 1-phenyl-3-(thiophen-3-yl)-1H- pyrazole-4-carboxylic acid and study of their anticancer activity
Inceler, Nazan,Yilmaz, Akin,Baytas, Sultan Nacak
, p. 3109 - 3118 (2013/07/11)
A series of novel thiophene containing 1,3-diarylpyrazole derivatives were synthesized and the structures were determined by IR, 1H-NMR, and HRMS analysis. The anticancer activity of the title compounds against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells growth were investigated by MTT assay. Interestingly, Raji and HL60 cells exhibited more sensitivity to synthesized compounds. (4-Benzyl-piperidin-1-yl)-(1-phenyl-3-thiophen-3-yl-1H- pyrazol-4-yl)-methanone (4c) possessed the highest growth inhibitory effect on Raji and HL60 cancer cells (GI50 25.2 ± 3.2 and 28.3 ± 1.53 μM, respectively). Compound 4f, 4-trifluoromethylphenyl piperazine at the amide part, also showed potent activity on Raji and HL60 cancer cell lines with a GI50 value of 32.0 ± 1.27 and 36.7 ± 2.15 μM, respectively. Physicochemical properties of the synthesized compounds were evaluated in silico, and it was found that all compounds should present good passive oral absorption. All synthesized compounds demonstrated good drug-likeness values. The data suggested that these compounds might be promising for further development.
Synthesis of 3-substituted 1-phenyl-1H-pyrazole-4-carbaldehydes and the corresponding ethanones by Pd-catalysed cross-coupling reactions
Arbaciauskiene, Egle,Martynaitis, Vytas,Krikstolaityte, Sonata,Holzer, Wolfgang,Sackus, Algirdas
experimental part, p. 1 - 21 (2012/02/04)
An efficient synthetic route to construct ortho-substituted 1-phenyl-1H-pyrazole-4-carboxaldehydes and the corresponding ethanones starting from 1-phenyl-1H-pyrazol-3-ol is described. Carbon-carbon bond-forming Pd-catalysed cross-coupling reactions were applied for the functionalisation of the intermediate pyrazole triflates. Detailed NMR spectroscopic investigations were undertaken with all obtained products. ARKAT-USA, Inc.
