Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro

A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a–x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a–x using microwave irradiation has been described. The effect of synthesized compounds 8a–v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.

A new series of benzofuran bearing pyrazolines was screened against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells.Figure optionsDownload as PowerPoint slideHighlights
► An efficient synthetic strategy to novel functionalized benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones through microwave irradiation has been reported.
► The newly synthesized benzofuran bearing pyrazoles have been screened for antiproliferative and MDR reversal activity in tumor cell lines and found potent active.
► The scope and generality of the present procedure is the easy workup process, short reaction time and high yield of the products with excellent purity.
► In addition, nowadays many research groups are working on the development of various synthetic methodologies for the synthesis of potent anticancer agents. Our present research plays vital role in this area and gives new way to explore biological utility of benzofuran bearing pyrazole molecules. Thus, the present methodology will be beneficial for many research groups in the synthetic organic chemistry as well in medicinal chemistry.