61277-58-5Relevant academic research and scientific papers
A Potent Glucose-Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells
Patra, Malay,Johnstone, Timothy C.,Suntharalingam, Kogularamanan,Lippard, Stephen J.
, p. 2550 - 2554 (2016)
Three rationally designed glucose-platinum conjugates (Glc-Pts) were synthesized and their biological activities evaluated. The Glc-Pts, 1-3, exhibit high levels of cytotoxicity toward a panel of cancer cells. The subcellular target and cellular uptake mechanism of the Glc-Pts were elucidated. For uptake into cells, Glc-Pt 1 exploits both glucose and organic cation transporters, both widely overexpressed in cancer. Compound 1 preferentially accumulates in and annihilates cancer, compared to normal epithelial, cells in vitro. Glucose-platinum conjugates for targeted delivery: A rationally designed potent glucose-platinum conjugate exploits glucose transporters, which are widely overexpressed in cancers, for internalization and selectively accumulates in and annihilates cancer cells.
COORDINATION COMPOUNDS, SYNTHESES, NANOFORMULATION AND USE THEREOF IN ONCOLOGY
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Page/Page column 23, (2018/06/21)
The present invention relates to mononuclear and dinuclear coordination compounds of Ru and Ga, pharmaceutical formulations based thereof, the relative method of synthesis and encapsulation of the compounds in macromolecules, supramolecular aggregates or
Glycosylated Platinum(IV) Complexes as Substrates for Glucose Transporters (GLUTs) and Organic Cation Transporters (OCTs) Exhibited Cancer Targeting and Human Serum Albumin Binding Properties for Drug Delivery
Ma, Jing,Wang, Qingpeng,Huang, Zhonglv,Yang, Xiande,Nie, Quandeng,Hao, Wenpei,Wang, Peng George,Wang, Xin
, p. 5736 - 5748 (2017/07/22)
Glycosylated platinum(IV) complexes were synthesized as substrates for GLUTs and OCTs for the first time, and the cytotoxicity and detailed mechanism were determined in vitro and in vivo. Galactoside Pt(IV), glucoside Pt(IV), and mannoside Pt(IV) were highly cytotoxic and showed specific cancer-targeting properties in vitro and in vivo. Glycosylated platinum(IV) complexes 5, 6, 7, and 8 (IC50 0.24-3.97 μM) had better antitumor activity of nearly 166-fold higher than the positive controls cisplatin (1a), oxaliplatin (3a), and satraplatin (5a). The presence of a hexadecanoic chain allowed binding with human serum albumin (HSA) for drug delivery, which not only enhanced the stability of the inert platinum(IV) prodrugs but also decreased their reduction by reductants present in human whole blood. Their preferential accumulation in cancer cells compared to noncancerous cells (293T and 3T3 cells) suggested that they were potentially safe for clinical therapeutic use.
D-Glucose and d-mannose-based metabolic probes. Part 3: Synthesis of specifically deuterated d-glucose, d-mannose, and 2-deoxy-d-glucose
Fokt, Izabela,Skora, Stanislaw,Conrad, Charles,Madden, Timothy,Emmett, Mark,Priebe, Waldemar
, p. 111 - 119 (2013/03/28)
Altered carbohydrate metabolism in cancer cells was first noted by Otto Warburg more than 80 years ago. Upregulation of genes controlling the glycolytic pathway under normoxia, known as the Warburg effect, clearly differentiates malignant from non-maligna
Synthesis of multivalent glucosides with high affinity for GLUT1 transporter
Qu, Boyi,Li, Xun,Wu, Jianbo,Li, Xiaolong,Hai, Li,Wu, Yong
scheme or table, p. 390 - 395 (2012/08/29)
The novel bifunctional compounds L1 and L2 carrying cluster glucosides as ligands for brain targeting liposomes were synthesized. 2-phenyl-1,3-dioxan-5-ol (8) and tetra-antennary alcohol (13) were used as the core scaffold to attach cholesterol derivatives by a triethylene glycol chain, while their remaining branches were linked with two or three benzylglucosides, which would be debenzvlated later to produce di-antennary glucosides L1 and tri-antennary glucosides ligand L2. This design provided an effective entry for the synthesized bifunctional compounds to cross blood brain barrier (BBB).
