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. 2019 Jun 4;12(2):84. doi: 10.3390/ph12020084

Table 1.

List of glycoconjugated prodrugs.

Aglycons Conjugated Sugars Response of Glycoconjugates Compared to Aglycon in In-Vitro or In-Vivo Transportation Mode Ref(s)
Chlorambucil Peracetylated 2-fluorodeoxyglucose Human fibroblasts, MCF-7 (25-fold more active) and Mice (Increased in MTD) - [57]
Docetaxel Glucose, galactose, mannose, xylose B16 murine melanoma cells (3 to 18-fold more active) - [58]
Docetaxel galactose Syngeneic P388 murine leukemia tumor model (equivalent) - [59]
Paclitaxel Glucose, glucuronic Acid HUV-EC-C and CHO-K1, NCI-H838, Hep-3B, A498, MES-SA, HCT-116, NPC-TW01, MKN-45 (All less toxic) Partially GLUT-1, /GLUT-3/GLUT-4 mediated [48,60]
Chlorambucil Amino derivatives of glucose, mannose, galactose, xylose, lyxose, D-threoside NCI-H460, A549, Du145, SKOV3, Hep3b, SF268, MCF7, HT29, HCT15, H1299 (induce decrease in cell growth) - [61]
Benzylguanine Glucose HeLa S3 and HeLa MR cells (inhibition of O6-methyl-guanine-DNA methyltransferase, MGMT) - [62]
Azomycin Glucose Several immortalized murine and human cancer cells (improved selectivity towards hypoxic tumor as radiosensitizer) GLUTs mediated [63]
Adriamycin 2-amino-2-deoxy-glucose MCF-7, Bel-7402, HepG2, MDA-MB-231, U87MG, HELF, SKOV3, and S180, HELF and mice (enhance selectivity towards cancer cells) GLUTs mediated [64]
Geldanamycin Glucose, lactose, galactose SW620, HT29, MCF7, K562 (one showed 3- to 40-fold enhanced activity with β-galactosidase) - [65]
Platinum Glucose DU145, RWPE2 GLUTs mediated [66]
Cadalene Glucose, lactose, galactose In vitro (less toxic) and in vivo (reduced tumor size) - [67]
Ketoprofen Glucose Cross blood−brain barrier (BBB) GLUTs mediated [68]
Nordihydroguaiaretic acid Galactose, glucose NCI/ADR-RES, Hep3B, MCF-7, HT-29 - [69]