Pharmacological Evaluation of New 4, 5-dihydro-1H- Pyrazole-1-yl acetate Derivatives as anti-cancer agents

Abstract

A series of nine novel 4, 5-dihydro-1H- pyrazole-1-yl acetate derivatives (IVa-i) by Shahlaa et al. was investigated in vitro for their antiproliferative activity against two cancer cell lines, breast cancer cell line (MCF-7) and lung cancer cell lines (A549), According to   the cytotoxicity effect of these compounds, IVa, IVc and IVi compounds have antiproliferative effect with percentage (81.30%, 87.4% & 54.66%) respectively at 72h treatment on MCF-7 cell line compared to other compounds, these results indicate that the new compound IVc have the higher antiproliferative percent comparable to tamoxifen as a standard anti-tumour for oestrogen receptor positive breast cancer cell line after 72h followed by IVa after 72h (83.31%). cytotoxicity effect of compound IVb was highest among tested compounds on lung cancer cell line (A549) with antiproliferative percentage (58.49% & 75.04%) at 48 & 72h respectively, but it is less than erlotinib as a standard anti-tumour for lung cancer cell line cytotoxicity effect (77.10% & 82.46%) at these times. three compounds (IVa, IVc & IVi) have antiproliferative effect on breast cancerous cell line (MCF-7) and compound (IVc) have inhibition percentage comparable to that of the authorized medication Tamoxifen. One compound (IVb) had antiproliferative activity, but less than that of erlotinib on lung cancerous cell line (A549) and there is good agreement between our docking results and the experimental results.