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rGO‐SO 3 H Catalysed Green Synthesis of Fluoro‐Substituted Aminomethylene Bisphosphonates and their Anticancer, Molecular Docking studies
Author(s) -
Sudileti Murali,
Nagaripati Saichaithanya,
Gundluru Mohan,
Chintha Venkataramaiah,
Aita Saikiran,
Wudayagiri Rajendra,
Chamarthi Nagaraju,
Cirandur Suresh Reddy
Publication year - 2019
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201903191
Subject(s) - chemistry , phosphonate , methylene , docking (animal) , trifluoromethyl , mtt assay , stereochemistry , combinatorial chemistry , in vitro , medicinal chemistry , organic chemistry , biochemistry , alkyl , medicine , nursing
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.