Publication: Novel 1-((benzoimidazole-2-yl)methyl)-3-phenyl- 1,4-dihydropyrazole-5-one and their derivatives: Synthesis and preliminary cytotoxicity test as anti-breast cancer
No Thumbnail Available
Date
2017
Journal Title
Journal ISSN
Volume Title
Publisher
American Scientific Publishers
Abstract
This work presented synthesis of new pyrazolone derivatives and their cytotoxicity assay. The synthesis of pyrazolone derivatives have been achieved using condensation of 2-hydrazinyl methyl-1H-benzoimidazole (H1) with ethylbenzoylacetate in presence of ethanol, which in turn, yielded 1-(benzoimidazole-2-yl)methyl-3-phenyl-1, 4-dihydropyrazole-5-one (BPP). Then, it has reacted with diazonium solution in ethanol and benzoyl chloride in hot dioxin to give 4-azo pyrazolone (BMPAP) and 4-acyl pyrazolone (BMPBP) respectively. The newly synthesized compounds were characterized by FT-IR, 1H NMR and13C NMR. The cytotoxicity assay of the BPP, BMPAP and BMPBP on human breast cancer cells (MCF7) demonstrated their killing ability similar with naturally occurring toxins or immune-mediator cells. The cytotoxicity test was performed using MTT assay (3-[4, 5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide). Cell culture with the concentration of 2�104 cells/ml was prepared and was plated (100 �l/well) onto 96-well plates. The diluted ranges of sample extracts were added to each well with identified concentrations: 100, 50, 25, 12.5, 6.25, 3.13 and 1.56 �g/ml and then incubated for 72 hr. MTT solution was added at the end of incubation samples to the cells and continued further for incubation in 3 hr. After solubilization of the purple formazan crystals using DMSO were completed, the Optical Density (OD) was measured using an ELISA reader at a wavelength of 570 nm. The cytotoxicity was recorded as the drug concentration causing 50% growth inhibition of the tumor cells (IC50 value). Overall cytotoxicity test was varied between pyrazolone derivatives with 50% or higher inhibition below 27 �g/ml, and it was considered active and potentially target for further screening. � 2017 American Scientific Publishers All rights reserved.
Description
Keywords
Anti-breast cancer, Cytotoxicity assay, Pyrazolone derivatives, Synthesis, Tumor cells