TY - JOUR
T1 - Oligosaccharides related to tumor‐associate antigens. Part 3. Synthesis of the propyl glycosides of the trisaccharide β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐(1→3)‐α‐D‐Galp and of the Tetrasaccharide α‐L‐Fucp‐(1→2)‐β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐(1→3)‐α‐D‐Galp, components of a tumor antigen recognized by the antibody MBr1
AU - Lay, Luigi
AU - Panza, Luigi
AU - Russo, Giovanni
AU - Colombo, Diego
AU - Ronchetti, Fiamma
AU - Adobati, Elena
AU - Canevari, Silvana
PY - 1995/5/10
Y1 - 1995/5/10
N2 - The synthesis of the trisaccharide β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐(1→3)‐α‐D‐Galp‐1‐OPr (2) and of the tetrasaccharide α‐L‐Fucp‐(1→2)‐β‐D‐GalpNAc‐(1→3)‐β‐D‐Galp‐1‐OPr (3), starting from the disaccharidic dihydrooxazole donor 5, is described. Glycosylation of 5 with 6 in the presence of Me3SiOTf gave the trisaccharide 7 which was deprotected with standard methods to give, via 8, compound 2 (Scheme 1). Alternatively, protection of 8 as the 4′,6′‐O‐benzylidene derivative 9 followed by glycosylation with 10 and by standard deprotection afforded the tetrasaccharide 3 (Scheme 2). Biological testing showed that trisaccharide 2 is unable to inhibit the binding of the monoclonal antibody MBr1 to the target tumor cells MCF7, while tetrasaccharide 3 inhibits the binding in ca. 7‐fold extent with respect to the previously tested trisaccharide α‐L‐Fucp‐(1→2)‐β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐1‐OPr. These results indicate that the galactose corresponding to the unit D of compound 1 plays an important role in defining the MBr1‐recognized epitope and confirm the essential role of fucose for MAb recognition.
AB - The synthesis of the trisaccharide β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐(1→3)‐α‐D‐Galp‐1‐OPr (2) and of the tetrasaccharide α‐L‐Fucp‐(1→2)‐β‐D‐GalpNAc‐(1→3)‐β‐D‐Galp‐1‐OPr (3), starting from the disaccharidic dihydrooxazole donor 5, is described. Glycosylation of 5 with 6 in the presence of Me3SiOTf gave the trisaccharide 7 which was deprotected with standard methods to give, via 8, compound 2 (Scheme 1). Alternatively, protection of 8 as the 4′,6′‐O‐benzylidene derivative 9 followed by glycosylation with 10 and by standard deprotection afforded the tetrasaccharide 3 (Scheme 2). Biological testing showed that trisaccharide 2 is unable to inhibit the binding of the monoclonal antibody MBr1 to the target tumor cells MCF7, while tetrasaccharide 3 inhibits the binding in ca. 7‐fold extent with respect to the previously tested trisaccharide α‐L‐Fucp‐(1→2)‐β‐D‐Galp‐(1→3)‐β‐D‐GalpNAc‐1‐OPr. These results indicate that the galactose corresponding to the unit D of compound 1 plays an important role in defining the MBr1‐recognized epitope and confirm the essential role of fucose for MAb recognition.
UR - http://www.scopus.com/inward/record.url?scp=0029076022&partnerID=8YFLogxK
U2 - 10.1002/hlca.19950780302
DO - 10.1002/hlca.19950780302
M3 - Article
SN - 0018-019X
VL - 78
SP - 533
EP - 538
JO - Helvetica Chimica Acta
JF - Helvetica Chimica Acta
IS - 3
ER -