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Baloxavir Acid-Induced Mitochondrial Toxicity and Cell Cycle Arrest Contribute to Its Adverse Effects. [PDF]
Int J Mol SciZhan P +6 more
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Fatty Acids in Cancer Therapy: Chemical Conjugates, Nanocarriers, and Therapeutic Opportunities. [PDF]
MoleculesAntal G +7 more
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Nucleophile-triggered prodrug release from polymer hydrogels.
RSC Appl PolymKlemm B +6 more
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Prodrugs in medicinal chemistry and enzyme prodrug therapies
Advanced Drug Delivery Reviews, 2017Prodrugs are cunning derivatives of therapeutic agents designed to improve the pharmacokinetics profile of the drug. Within a prodrug, pharmacological activity of the drug is masked and is recovered within the human body upon bioconversion of the prodrug, a process that is typically mediated by enzymes.
Raoul Walther +2 more
exaly +3 more sources
Bioorganic & Medicinal Chemistry Letters, 1998
A photolabile derivative (1) of the anticancer drug, 5-fluorodeoxyuridine (2), was designed and synthesized as a model prodrug. Photolysis of 1 with long-wavelength UV light rapidly released 2 in solution. While compound 1 alone is nontoxic to cells, the presence of both 1 and UV irradiation (lambda = 350 nm) resulted in potent inhibition of cell ...
Y, Wei, Y, Yan, D, Pei, B, Gong
openaire +2 more sources
A photolabile derivative (1) of the anticancer drug, 5-fluorodeoxyuridine (2), was designed and synthesized as a model prodrug. Photolysis of 1 with long-wavelength UV light rapidly released 2 in solution. While compound 1 alone is nontoxic to cells, the presence of both 1 and UV irradiation (lambda = 350 nm) resulted in potent inhibition of cell ...
Y, Wei, Y, Yan, D, Pei, B, Gong
openaire +2 more sources
International Journal of Pharmaceutics, 2004
In 1975 Prof. H. Ringsdorf proposed a model for rational design of polymeric prodrugs [J. Polym. Sci. Symp. 51 (1975) 135]. The model has been the most important basis for research in the field, since it was the first model that took into account both the chemical and biological aspects needed for the design of polymeric prodrugs. This paper deals with
K, Hoste, K, De Winne, E, Schacht
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In 1975 Prof. H. Ringsdorf proposed a model for rational design of polymeric prodrugs [J. Polym. Sci. Symp. 51 (1975) 135]. The model has been the most important basis for research in the field, since it was the first model that took into account both the chemical and biological aspects needed for the design of polymeric prodrugs. This paper deals with
K, Hoste, K, De Winne, E, Schacht
openaire +2 more sources
1993
To exert its antitumor effects, leucovorin must ultimately become activated by conversion to CH2FH4.* Elevation of this reduced folate cofactor stabilizes the inhibitory ternary complex formed between the FU active metabolite, FdUMP and thymidylate synthase, resulting in suppression of DNA synthesis or repair.1–4 It has been demonstrated both in animal
D G, Priest, J C, Schmitz, T, Walle
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To exert its antitumor effects, leucovorin must ultimately become activated by conversion to CH2FH4.* Elevation of this reduced folate cofactor stabilizes the inhibitory ternary complex formed between the FU active metabolite, FdUMP and thymidylate synthase, resulting in suppression of DNA synthesis or repair.1–4 It has been demonstrated both in animal
D G, Priest, J C, Schmitz, T, Walle
openaire +2 more sources
Current Medicinal Chemistry, 2002
Bisphosphonates (BP) are pyrophosphate analogs having a P-C-P backbone. The oral bioavailability of BPs is ca. 1%, due to high ionisation at physiological pH. Using the prodrug approach, oral absorption can be increased by masking one or more ionizable groups (clodronate, etidronate), or using a targeting carrier system (alendronate, pamitronate).
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Bisphosphonates (BP) are pyrophosphate analogs having a P-C-P backbone. The oral bioavailability of BPs is ca. 1%, due to high ionisation at physiological pH. Using the prodrug approach, oral absorption can be increased by masking one or more ionizable groups (clodronate, etidronate), or using a targeting carrier system (alendronate, pamitronate).
openaire +2 more sources