Results 211 to 220 of about 20,922 (255)
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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
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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
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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
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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
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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).
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Il Farmaco, 1999
An overview of the different heterocyclic NO-releasing compounds is given. Mesoionic heterocycles like sydnone imines are one example. This class is discussed on the synthesis and the mechanism of NO formation from Molsidomine and its first metabolite SIN-1.
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An overview of the different heterocyclic NO-releasing compounds is given. Mesoionic heterocycles like sydnone imines are one example. This class is discussed on the synthesis and the mechanism of NO formation from Molsidomine and its first metabolite SIN-1.
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Prodrugs in Cancer Chemotherapy
Xenobiotica, 1986At present, chemotherapy is not very effective against common solid cancers especially once they have metastasised. However, laboratory experiments and studies on dose intensification in humans have indicated that some anti-cancer agents might be curative but only if the dose given was very much higher than that presently obtainable clinically ...
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2023
A Prodrug is a specialized substance designed to contain the parent drug while remaining either inactive or only partially active. These molecules are intentionally engineered to undergo biotransformation within the body, either through chemical or enzymatic cleavage, in order to release the active compound at levels suitable for therapeutic effects ...
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A Prodrug is a specialized substance designed to contain the parent drug while remaining either inactive or only partially active. These molecules are intentionally engineered to undergo biotransformation within the body, either through chemical or enzymatic cleavage, in order to release the active compound at levels suitable for therapeutic effects ...
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Activation of Prodrugs Depend on the Metabolism of These Prodrugs
Current Research in Medical SciencesProdrugs depend on enzymatic processes, essentially in the liver, but can also occur in other tissues to release the active metabolite. These metabolic biotransformations are often enzymatically controlled, ensuring the drug becomes pharmacologically active at its site of action.
Rezk R. Ayyad +5 more
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