201210-70-0Relevant articles and documents
Selective bone targeting 5-fluorouracil prodrugs: Synthesis and preliminary biological evaluation
Ouyang, Liang,He, Dongsheng,Zhang, Jing,He, Gu,Jiang, Bo,Wang, Qiang,Chen, Zhengjun,Pan, Junzhu,Li, Yanhua,Guo, Li
, p. 3750 - 3756 (2011)
Bone tumor is a notoriously difficult disease to manage, requiring frequent and heavy doses of systemically administered chemotherapy. Targeting anticancer drug to the bone after systemic administration may provide both greater efficacy of treatment and l
Self-assembly of a 5-fluorouracil-dipeptide hydrogel
Sun, Yuan,Kaplan, Jonah A.,Shieh, Aileen,Sun, Hui-Lung,Croce, Carlo M.,Grinstaff, Mark W.,Parquette, Jon R.
, p. 5254 - 5257 (2016/05/02)
The self-assembly of 5-fluorouracil dilysine conjugates into self-supporting hydrogels, comprised of entangled nanofibers or rigid nanotubes with diameters of 10 and 16 nm, respectively, is reported. The rate of release of 5-Fu from the conjugates was highly dependent on concentration in solution, whereas, release from the fully formed hydrogels was significantly slower. The 5-Fu conjugate also exhibited promising in vitro cytotoxicity against human tumor cell lines A549, H460 and H23.
SELF-ASSEMBLY OF THERAPEUTIC AGENT-PEPTIDE NANOSTRUCTURES
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Paragraph 0189, (2014/06/23)
Disclosed are conjugates of hydrophobic drugs linked to protected or unprotected amino acids or peptides. The disclosed conjugates are amphiphilic and can self assemble into nanotubes. Nanotubes comprising the conjugates are also described and can have hi
Synthesis and characterization of new liver targeting 5-fluorouracil-cholic acid conjugates
Qian, Shan,Wu, Jian-Bo,Wu, Xiao-Chun,Li, Jie,Wu, Yong
experimental part, p. 513 - 520 (2009/12/24)
The objective of this work was to develop a liver-specific antihepato carcinoma agent. A series of 5-fluorouracil / cholic acid conjugates (5-FU-cholic acid conjugates) were prepared and tested for their chemical characteristics and bio-distribution properties. The in-vitro stability trial showed 5-FU-cholic acid conjugates could be completely hydrolyzed by heating at 70°C in an acidic solution, pH = 1, for 5 min. The fast and complete hydrolysis of these compounds could be compatible with a fast separation and analysis method to shorten the analysis time. The decomposition speeds of the 5-FU-cholic acid conjugates in different organs of mice at several time points after oral administration were evaluated by measuring the concentrations of regenerated 5-FU in organ tissue. The results were compared with those of the controls, which was a group of mice orally taking 5-FU. The concentrations of 5-FU in mice liver tissue were remarkably increased after oral administration of the prodrugs, and were much larger than if only orally administered 5-FU. The results suggested the feasibility to improve therapeutic efficiency of liver targeting treatments by using cholic acid as the vector of drugs.
Synthesis and cytotoxicity of 5-fluorouracil/diazeniumdiolate conjugates
Cai, Tingwei Bill,Tang, Xiaoping,Nagorski, Janet,Brauschweiger, Paul G.,Wang, Peng George
, p. 4971 - 4975 (2007/10/03)
5-Fluorouracil/diazeniumdiolate conjugates were first synthesized, and showed greater cytotoxicities than 5-fluorouracil for DU 145 human prostate and HeLa cancer cells.
Synthesis and reactivity of 5-fluorouracil/cytarabine mutual prodrugs
Menger, Fredric M.,Rourk, Michael J.
, p. 9083 - 9088 (2007/10/03)
Two mutual prodrugs, in which two different anti-cancer drugs are attached to the same molecule via labile linkages, are synthesized and examined kinetically. One of the mutual prodrugs loses a drug component under physiological conditions within an hour, but the other mutual prodrug (having a longer spacer between the two drugs) is stable to chemical degradation even at hither pH values. Thus, enzymatic hydrolysis alone will release the two anti-cancer drugs. The potential value of anti-cancer mutual prodrugs is discussed.
