title: Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 2.
abstract: A series of novel phosphinates, derived from 4-phosphonomethylphenylalanine, are described as isosteres of phosphotyrosine. Benzyl (or alkyl) phosphinomethylphenylalanine derivatives were prepared by alkylation of an amino acid P-H phosphinate.
authors.affiliation: Novartis Horsham Research Centre, West Sussex, UK. clive.walker@pharma.novartis.com
authors.forename: C V
authors.initials: CV
authors.lastname: Walker
authors.forename: G
authors.initials: G
authors.lastname: Caravatti
authors.forename: A A
authors.initials: AA
authors.lastname: Denholm
authors.forename: J
authors.initials: J
authors.lastname: Egerton
authors.forename: A
authors.initials: A
authors.lastname: Faessler
authors.forename: P
authors.initials: P
authors.lastname: Furet
authors.forename: C
authors.initials: C
authors.lastname: García-Echeverría
authors.forename: B
authors.initials: B
authors.lastname: Gay
authors.forename: E
authors.initials: E
authors.lastname: Irving
authors.forename: K
authors.initials: K
authors.lastname: Jones
authors.forename: A
authors.initials: A
authors.lastname: Lambert
authors.forename: N J
authors.initials: NJ
authors.lastname: Press
authors.forename: J
authors.initials: J
authors.lastname: Woods
mesh_terms: D048868:Adaptor Proteins, Signal Transducing; D000596:Amino Acids; D015195:Drug Design; D051380:GRB2 Adaptor Protein; D015394:Molecular Structure; D010649:Phenylalanine / Q000031:analogs & derivatives*; D010721:Phosphinic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019000:Phosphotyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D011506:Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship; D018909:src Homology Domains
chemical_list: D048868:Adaptor Proteins, Signal Transducing; D000596:Amino Acids; D051380:GRB2 Adaptor Protein; D010721:Phosphinic Acids; D011506:Proteins; C083973:4-phosphonomethylphenylalanine; D019000:Phosphotyrosine; D010649:Phenylalanine