Synthesis, Characterization and In-Vitroanti-Tumor Activity of Some Novel Pyrazole Derivatives

Abstract

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as a potent anti-inflammatory, antipsychotic , anti-obesity drug, an analgesic, and anti-depressant agents have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This heterocyclic can be traced in a number of well-established drugs belonging to different categories with diverse therapeutic activities. Aim of the present study is to synthesize and characterize various 4-[1-(2-hydroxy-4,4-dimethyl-6-oxocyclohex-1-en-1-yl)3,4-(phenyl]-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one derivatives using an efficient Scheme. The synthesized compounds (1-10) were evaluated for their in vitro anti-cancer activity.In order to develop potent anti-cancer agents, a novel series of pyrazole derivatives were synthesized and the structures of all compounds were confirmed by spectral studies. MTT assay has been employed to study anti-proliferative activity of these compounds with four human cancer cell lineDLD1 (Human Colorectal Adenocarcinoma) at various concentration (6.25-100µg/mL). The results revealed that compounds VEPD and 4MEPD shows goodanti-tumoractivity and the other compounds shows moderate activity against theDLD1cell line.