Glycoconjugation: An approach to cancer therapeutics

Table 1 List of the glycoconjugates and its effects

Agent	Activity	Sugar moiety	Efficacy glycoconjugates compared to aglicone
Ifosfamide	Alkalating agent	Glucose	In vitro (less toxic) and in vivo (reduced tumor size). Clinical trials ongoing.
Chlorambucil	Alkalating and DNA-complexing agent	D-threose	HT29 and HCT15 (showed 8-12 fold, and 15-fold, respectively, improved activities targeting cancers cell lines over the parent drug).
Geldanamycin	HSP90 inhibitor	Glucose	Glucose-GA showed anticancer activity with IC50 of 70.2-380.9 nM in SW620, HT29, MCF-7 and K562 cancer cells by-glucosidase activation inside of the tumor cells.
Geldanamycin	HSP90 inhibitor	Galactose	SW620, HT29, MCF-7 and K562 (anticancer activity of galactose-GE conjugate increased by 3- to 40-fold when incubated with galactosidase over the parent drug).
Emodin	Tyrosine kinase inhibitor	D-rhamnose	A594, HepG2, OVCAR-3, Hela, K562 and SGC-790 (cell proliferation was inhibited and EM-d-Rha conjugate displayed IC50 values in low μmolar ranges).
Paclitaxel	Mitotic inhibitor	Glucose	NCl-H838, MES-SA, HCT-116, and NPC-TW01 (cell proliferation was inhibited the conjugated presented higher cytotoxicity, induced tubulin aggregation and chromosomal condensation compared to paclitaxel).
Doxorubicin	Antitumor antibiotic	Galactose	In vitro viability of HepG2 (hepatocarcinoma) and MCF-7 (breast cancer) tumor cells incubated with DOX was higher than that of Gal-DOX. In vivo experiments showed that tumor size in Gal-DOX-treated groups was greatly reduced in comparison to the DOX-treated group.
Doxorubicin	Antitumor antibiotic	2-amino-2-deoxy-D-glucose and succinic acid	In vitro and in vivo studies showed that 2DG-SUC-ADM induced a higher level of apoptosis and higher inhibition rates in MCF-7 and HepG2 tumoral cells than the parent aglycone ADM.