87995-78-6Relevant academic research and scientific papers
Some 1,3,5-trisubstituted pyrazoline derivatives targeting breast cancer: Design, synthesis, cytotoxic activity, EGFR inhibition and molecular docking
El Kerdawy, Ahmed M.,El-Ansary, Dina Y.,George, Riham F.,Kandeel, Manal
, (2020/03/31)
Different 1,3,5-trisubstituted pyrazoline derivatives 2a-c, 3-c, 4a-f, 6a-c, 7a-f and 8a-d were prepared via condensation reaction of the appropriate chalcone 1a-c or 5a-c with various hydrazine derivatives. All compounds were screened for their cytotoxicity against breast MCF-7 cancer cell line and the normal fibroblasts WI-38. Thirteen compounds 2a, 3a, 3c, 4a-d, 6c, 7d, 7e, 8b, 8d and 8f revealed promising cytotoxicity against MCF-7 compared to the reference standard staurosporine and they were safe to the normal fibroblasts WI-38. In addition, compounds 3c, 6c, 7d, 8b and 8d elicited higher cytotoxicity than erlotinib and exhibited promising EGFR inhibitory activity at submicromolar level comparable to that of erlotinib except for compound 8b that may exert its cytotoxicity via another mechanism besides EGFR inhibition. Molecular docking of 3c, 6c, 7d, 8b and 8d in the active site of EGFR confirmed the obtained results.
Antibacterials and antimycotics: Part 1: Synthesis and activity of 2- pyrazoline derivatives
Nauduri, Dhananjaya,Reddy, Gopu Bala Show
, p. 1254 - 1260 (2007/10/03)
A series of 3-styryl-1,5-diphenyl and 5-styryl-1,3-diphenyl 2- pyrazolines of different substitutions has been synthesized by condensation of substituted α,β-unsaturated ketones with phenylhydrazine hydrochloride in presence of catalytic amount of concentrated HCl. Compounds in the 3- styryl series had OMe, NMe2, NO2, OH and isopropyl substituents and those in the 5-styryl series had OMe, NMe2 and NO(s). The 3-styryl-1,5-diphenyl compounds showed little variation in antibacterial activity towards gram- positive and gram-negative bacteria in terms of geometric mean minimum inhibitory concentrations (MIC). The 4',4-NMe2, 4',4-NO2 and 4',4-OMe compounds were found to possess the highest activity in the series. The 5- styryl-1,3-diphenyl series showed lower activities than the 3-styryl series. The in vitro antimycotic activity of the 4',4-OH and 2',2-OH substituted compounds showed good activity than the other molecules in the two series.
1,3-Dipolar Cycloadditions, 90. Diphenylnitrilimine and Substituted Butadienes; Substituent Effects and Rate of Cycloaddition
Fliege, Werner,Huisgen, Rolf,Kolbeck, Winfried,Weberndoerfer, Volkmar
, p. 3438 - 3460 (2007/10/02)
1-Substitued butadienes accept diphenylnitrilimine (2) not at the 1,2- but rather at the 3,4-double bond; the regiospecific cycloaddition furnishes 5-substituted 1,3-diphenyl-2-pyrazolines.The relative addition rates, measured in competition experiments,
