Results 21 to 30 of about 20,922 (255)

Lipophilic Nucleoside Triphosphate Prodrugs of Anti‐HIV Active Nucleoside Analogs as Potential Antiviral Compounds

open access: yesAdvanced Science, 2023
Nucleoside analogs require three phosphorylation steps catalyzed by cellular kinases to give their triphosphorylated metabolites. Herein, the synthesis of two types of triphosphate prodrugs of different nucleoside analogs is disclosed.
Xiao Jia, Dominique Schols, Chris Meier
doaj   +1 more source

Cyclooxygenase-Inhibiting Platinum(IV) Prodrugs with Potent Anticancer Activity

open access: yesPharmaceutics, 2022
Platinum(IV) prodrugs of the [Pt(PL)(AL)(COXi)(OH)]2+ type scaffold (where PL is 1,10-phenanthroline or 5,6-dimethyl-1,10-phenanthroline, AL is 1S,2S-diaminocyclohexane, and COXi is a COX inhibitor, either indomethacin or aspirin) were synthesised and ...
Aleen Khoury   +6 more
doaj   +1 more source

Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors

open access: yesMolecules, 2016
In this study, we report on the design, synthesis, photokinetic properties and in vitro evaluation of photoactivatable caged prodrugs for the receptor tyrosine kinase VEGFR-2.
Boris Pinchuk   +4 more
doaj   +1 more source

Can the Union of Prodrug Therapy and Nanomedicine Lead to Better Cancer Management?

open access: yesAdvanced NanoBiomed Research, 2022
Prodrug‐mediated and nanomedicine‐mediated therapies stand at the forefront of cancer management today. However, a lot of recent research efforts have been focused on identifying novel strategies in treating tumor by combining the techniques and ...
Giredhar Muthiah, Amit Jaiswal
doaj   +1 more source

Ex vivo mass spectrometry-based biodistribution analysis of an antibody-Resiquimod conjugate bearing a protease-cleavable and acid-labile linker

open access: yesFrontiers in Pharmacology, 2023
Immune-stimulating antibody conjugates (ISACs) equipped with imidazoquinoline (IMD) payloads can stimulate endogenous immune cells to kill cancer cells, ultimately inducing long-lasting anticancer effects.
Lydia Bisbal Lopez   +15 more
doaj   +1 more source

Cyclization-activated Prodrugs [PDF]

open access: yesMolecules, 2007
Many drugs suffer from an extensive first-pass metabolism leading to druginactivation and/or production of toxic metabolites, which makes them attractive targets forprodrug design. The classical prodrug approach, which involves enzyme-sensitive covalentlinkage between the parent drug and a carrier moiety, is a well established strategy toovercome ...
Paula Gomes, Nuno Vale, Rui Moreira
openaire   +5 more sources

Synthesis of 4′-Substituted Carbocyclic Uracil Derivatives and Their Monophosphate Prodrugs as Potential Antiviral Agents

open access: yesViruses, 2023
Over the past decades, both 4′-modified nucleoside and carbocyclic nucleoside analogs have been under the spotlight as several compounds from either family showed anti-HIV, HCV, RSV or SARS-CoV-2 activity.
Nicolas G. Biteau   +8 more
doaj   +1 more source

Toxicology and Biodistribution Studies for MGH2.1, an Oncolytic Virus that Expresses Two Prodrug-activating Genes, in Combination with Prodrugs

open access: yesMolecular Therapy: Nucleic Acids, 2013
MGH2.1 is a herpes simplex virus type 1 (HSV1) oncolytic virus that expresses two prodrug-activating transgenes: the cyclophosphamide (CPA)-activating cytochrome P4502B1 (CYP2B1) and the CPT11-activating secreted human intestinal carboxylesterase (shiCE).
Kazue Kasai   +9 more
doaj   +1 more source

The Feasibility of Enzyme Targeted Activation for Amino Acid/Dipeptide Monoester Prodrugs of Floxuridine; Cathepsin D as a Potential Targeted Enzyme

open access: yesMolecules, 2012
The improvement of therapeutic efficacy for cancer agents has been a big challenge which includes the increase of tumor selectivity and the reduction of adverse effects at non-tumor sites.
Gordon L. Amidon, Yasuhiro Tsume
doaj   +1 more source

Synthesis and Antiviral Activity of a Series of 2′-C-Methyl-4′-thionucleoside Monophosphate Prodrugs

open access: yesMolecules, 2020
The NS5B RNA-dependent RNA polymerase of the hepatitis C virus (HCV) is a validated target for nucleoside antiviral drug therapy. We endeavored to synthesize and test a series of 4′-thionucleosides with a monophosphate prodrug moiety for their antiviral ...
Zackery W. Dentmon   +2 more
doaj   +1 more source

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