74906-27-7Relevant academic research and scientific papers
One-Pot Synthesis and Antiproliferative Activity of Highly Functionalized Pyrazole Derivatives
Lusardi, Matteo,Rotolo, Chiara,Ponassi, Marco,Iervasi, Erika,Rosano, Camillo,Spallarossa, Andrea
, (2022/02/05)
A series of highly functionalized pyrazole derivatives has been prepared by a one-pot, versatile and regioselective procedure. Pyrazoles 1–29 were tested in cell-based assay to assess their antiproliferative activity against a panel of tumour cells. Addit
Synthesis, antitumor activity, enzyme assay, DNA binding and molecular docking of Bis-Schiff bases of pyrazoles
Morsy, Nesrin M.,Hassan, Ashraf S.,Hafez, Taghrid S.,Mahran, Mohamed R. H.,Sadawe, Inass A.,Gbaj, Abdul M.
, p. 47 - 59 (2020/07/27)
A novel series of Bis-Schiff bases of pyrazoles 9–24 were synthesized by the direct condensation of 5-aminopyrazoles 4a–d with dialdehydes 8a–d in ethanol. The newly synthesized Bis-Schiff bases of pyrazoles 9–24 were characterized and confirmed by analyt
Design, synthesis and antibacterial activity of N-aryl-3-(arylamino)-5-(((5-substituted furan-2-yl)methylene)amino)-1H-pyrazole-4-carboxamide as nitrofurantoin analogues
Hassan, Ashraf S.,Moustafa, Gaber O.,Morsy, Nesrin M.,Abdou, Amr M.,Hafez, Taghrid S.
, p. 4469 - 4481 (2020/12/09)
Nitrofurantoin is an effective drug and used for treating urinary infectious diseases. A series of nitrofurantoin analogues bearing furan and pyrazole scaffolds as N-aryl-3-(arylamino)-5-(((5-substituted furan-2-yl)methylene)amino)-1
V2O5/SiO2 as an efficient catalyst in the synthesis of 5-amino-pyrazole derivatives under solvent free condition
Khatab, Tamer K.,Hassan, Ashraf S.,Hafez, Taghrid S.
, p. 135 - 142 (2019/03/21)
An efficient and facile approach for the synthesis of 5-aminopyrazoles from ketene S,N-acetal and hydrazine hydrate via catalytic reaction under solvent free condition has been described. V2O5/SiO2 as a heterogeneous catalyst was prepared and characterize
Design, synthesis and biological evaluation of certain CDK2 inhibitors based on pyrazole and pyrazolo[1,5-a] pyrimidine scaffold with apoptotic activity
Ali, Ghada M.E.,Ibrahim, Diaa A.,Elmetwali, Amira M.,Ismail, Nasser S.M.
, p. 1 - 14 (2019/01/26)
Different series of novel pyrazole and pyrazolo[1,5-a] pyrimidine derivatives (2a-g), (3a-c), (7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit CDK2/cyclin A2 enzyme in vitro. In addition, the cytotoxicity of the newly synthesized compounds was screened against four different human cancer cell lines. The CDK2/cyclin A2 enzyme inhibitory activity revealed that compounds (2d) and (2 g) are among the most active with inhibitory activity values of 60% and 40%, respectively, while compounds (7d) and (10b) exhibited the highest activity among the newly synthesized derivatives against four tumor cell lines (HepG2, MCF-7, A549 and Caco2) with IC50 values 24.24, 14.12, 30.03 and 29.27 μM and 17.12, 10.05, 29.95 and 25.24 μM, respectively. Flow cytometry cell cycle assay was carried for compounds (7d) and (10b) to investigate their apoptotic activity. The obtained results revealed that they induced cell-cycle arrest in the G0-G1phase and reinforced apoptotic DNA fragmentation. Molecular modeling studies have been carried out to gain further understanding the binding mode of the target compounds together with field alignment to define the similar field properties.
