Abstract:
The QSAR model were successfully developed to calculate biological activity of
3, 5 di-substituted Pyrazoline derivatives as anticancer agents against AsPC-1 human
pancreatic cell line and U251 human glioblastoma cell line, a good correlation models
were obtained with R2=74.30% and R2=75.92% respectively, compounds (5-(4-
bromophenyl)-3-(4-nitrophenyl)-4,5-dihydro-1H-pyrazole) and (N, N-dimethyl-4-[3-
(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-5-yl] aniline) were found to be the most
effective anticancer agent against AsPC-1 and U251 cell lines, with IC50 values
0.31mM and 0.062mM respectively.
Series of 3, 5 di-substituted Pyrazoline derivatives were successfully synthesized
in two steps under solvent free condition, which verify one of goals of green
chemistry is the use of less hazardous solvents. Step one was synthesized enone by
condensing aldehyde with ketone via sodium hydroxide according to Claisen-Schmidt
condensation. Step two was a nucleophilic addition of hydrazine hydrate to enon. The
structures of these compounds have been elucidated by infra red, ultra violet, thin lyer
chromatography and Melting Point.