89145-06-2Relevant academic research and scientific papers
Synthesis of novel thiophene fused pyrazoline-thiocyanatoethanone derivative: Spectral, DFT, pharmacological, docking and in vitro antibacterial studies
Saranya,Murugavel
, (2021)
Novel thiophene fused pyrazoline-thiocyanatoethanone compound was synthesized with good yield. The synthesized compound molecular structure was authenticated by SCXRD. The spectral studies of the compound were recorded through NMR, FTIR and UV to ascertai
Reductive Ring-Opening 1,3-Difunctionalizations of Arylcyclopropanes with Sodium Metal
Wang, Shuo,Kaga, Atsushi,Yorimitsu, Hideki
supporting information, p. 219 - 223 (2020/11/04)
Sodium dispersion promotes reductive ring opening of arylcyclopropanes. The presence of a reduction-resistant electrophile, such as methoxypinacolatoborane, epoxide, oxetane, paraformaldehyde, or chlorotrimethylsilane, during the reductive ring opening event leads to the formation of 1,3-difunctionalized 1-arylalkanes by immediate trappings of the resulting two reactive carbanions. In particular, the ring-opening 1,3-diborylations of arylcyclopropanes afford 1,3-diborylalkanes with high syn selectivity.
Pyrazoline derivatives as tubulin polymerization inhibitors with one hit for Vascular Endothelial Growth Factor Receptor 2 inhibition
Yang, Bing,Zhou, Jiahua,Wang, Fa,Hu, Xiao-Wei,Shi, Yujun
, (2021/07/13)
In this work, to check the effect of the transposition of the rings in typical patterns, a series of pyrazoline derivatives 3a-3t bearing the characteristic 3,4,5-trimethoxy phenyl and thiophene moieties were synthesized and evaluated as tubulin polymeriz
Synthesis and Biological Evaluation of Pyrazoline and Pyrrolidine-2,5-dione Hybrids as Potential Antitumor Agents
Anisimova, Natalia Y.,Choe, Jun-yong,Lavecchia, Antonio,Loiodice, Fulvio,Meyer-Almes, Franz-Josef,Pokrovsky, Vadim S.,S Ramaa, C.,Smirnova, Galina B.,Sokolova, Darina V.,Spirina, Tatiana S.,Tilekar, Kalpana,Upadhyay, Neha
, p. 1813 - 1825 (2020/09/07)
In search of novel and effective antitumor agents, pyrazoline-substituted pyrrolidine-2,5-dione hybrids were designed, synthesized and evaluated in silico, in vitro and in vivo for anticancer efficacy. All the compounds exhibited remarkable cytotoxic effects in MCF7 and HT29 cells. The excellent antiproliferative activity toward MCF7 (IC50=0.78±0.01 μM), HT29 (IC50=0.92±0.15 μM) and K562 (IC50=47.25±1.24 μM) cell lines, prompted us to further investigate the antitumor effects of the best compound S2 (1-(2-(3-(4-fluorophenyl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl)pyrrolidine-2,5-dione). In cell-cycle analysis, S2 was found to disrupt the growth phases with increased cell population in G1/G0 phase and decreased cell population in G2/M phase. The excellent in vitro effects were also supported by inhibition of anti-apoptotic protein Bcl-2. In vivo tumor regression studies of S2 in HT29 xenograft nude mice, exhibited equivalent and promising tumor regression with maximum TGI, 66 % (i. p. route) and 60 % (oral route) at 50 mg kg?1 dose by both the routes, indicating oral bioavailability and antitumor efficacy. These findings advocate that hybridization of pyrazoline and pyrrolidine-2,5-dioes holds promise for the development of more potent and less toxic anticancer agents.
SOCl2 catalyzed cyclization of chalcones: Synthesis and spectral studies of some bio-potent 1H pyrazoles
Ranganathan, Kaliyaperumal,Suresh, Ramamoorthy,Vanangamudi, Ganesan,Thirumurthy, Kannan,Mayavel, Perumal,Thirunarayanan, Ganesamoorthy
, p. 271 - 288 (2014/06/24)
Some aryl-aryl 1H pyrazoles have been synthesised by cyclization of aryl chalcones and hydrazine hydrate in the presence of SOCl2. The yields of the pyrazoles are more than 85%. These pyrazoles are characterized by their physical con
Synthesis and structural studies of isomeric Δ2- pyrazolines
Ingle,Doshi,Raut
experimental part, p. 1517 - 1520 (2011/10/13)
1-(2′-Thienyl)-3-(4″-dimethylamino phenyl)-2-propen-1-one(la-e) react with hydrazine hydrochloride in DMF medium to give isomeric 1-H pyrazolines (lla-e), react with phenyl hydrazine hydrochloride in DMF medium to give isomeric 1 -phenyl pyrazolines (Illa
Synthesis of and pharmacological studies on the antidepressant and anticonvulsant activities of some 1,3,5-trisubstituted pyrazolines
Ruhoglu, Ozan,Oezdemir, Zuhal,Calis, Uensal,Guemuesel, Buelent,Bilgin, Abdullah Altan
, p. 431 - 436 (2007/10/03)
Eighteen 1-phenyl-, 1-thiocarbamoyl- and 1-N-substitutedthiocarbamoyl-3- phenyl-5-heteroaryl-2-pyrazoline derivatives were synthesized and tested for their antidepressant and anticonvulsant activities. Their chemical structures were proved by spectral and microanalysis. The antidepressant activities of the compounds were investigated by the "forced swimming test". Results showed that compounds II-a,b,c, III-1b,1c,4a showed activities equivalent to or higher than pargyline hydrochloride (CAS 306-07-0) and tranylcypromine sulfate (CAS 13492-01-8) that were used as reference antidepressant drugs. Anticonvulsant activities of the compounds were determined by maximal electroshock seizure (MES), subcutaneous metrazol (ScMet.) and rotarod toxicity tests in mice according to the phase I tests of the Antiepileptic Drug Development programme. Compounds I-a, II-a,b,c, III-1b,2a,2c were found protective against MES and III-1b,1c,2a,2c were found protective against ScMet. ECV · Editio Cantor Verlag.
Heterocycles. 3. Synthesis and Spectral Data of Some 2-Pyrazolines
El-Rayyes, Nizar R.,Hovakeemian, George H.,Hmoud, Hayat S.
, p. 225 - 229 (2007/10/02)
The reaction of 1,3-diaryl-2-propen-1-ones (Ia-o) with hydrazine and methyl- and phenylhydrazine produced different substituted 2-pyrazolines (III).The structures of these products were evident from their chemical and spectroscopic analysis.
