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A facile and green synthetic protocol was aimed for the synthesis of aminomethylene bisphosphonates via one-pot reaction of fluorine bearing anilines, triethyl orthoformate and dialkyl phosphite in presence of rGO-SO 3 H as catalyst under microwave irradiation and solvent-free conditions. All the title compounds were evaluated for their anticancer activity against human breast cancer cell lines (MCF-7) by MTT assay method using exemestane as standard drug. Molecular docking studies were carried out against Human estrogen receptor alpha (ERα). Both in vitro and in silico studies revealed that compounds tetramethyl (((3-(trifluoromethyl) phenyl) aminomethylene)bisphosphonate) (4e), tetramethyl (((2-methoxy(5-trifluoromethyl) phenyl) amino) methylene)bis (phosphonate) (4m) and tetraethyl (((4-bromo-2-fluorophenyl) amino)methylene)bis(phosphonate) (4l) exhibited remarkable higher anticancer activity than that of standard.

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