One-Pot Synthesis and Antiproliferative Activity of Highly Functionalized Pyrazole Derivatives

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. Additionally, the cytotoxicity of prepared compounds was evaluated against normal human fibroblasts. The antiproliferative activity of the synthesized molecules emerged to be affected by the nature of the substituents of the pyrazole scaffold and derivatives 21-23 proved to inhibit the growth of melanoma and cervical cancer cells. Compound 23 was identified as the most active derivative and docking simulations predicted its ability to interact with estrogen receptors.

Automated summary

A series of highly functionalized pyrazole derivatives were synthesized through a one-pot, versatile, and regioselective procedure. These derivatives exhibited antiproliferative activity against tumor cells, with compounds 21-23 showing inhibition of melanoma and cervical cancer cell growth. Compound 23 was identified as the most active derivative and was predicted to interact with estrogen receptors through docking simulations.