The expanding role of prodrugs in contemporary drug design and development

J Rautio, NA Meanwell, L Di… - Nature reviews drug …, 2018 - nature.com
Prodrugs are molecules with little or no pharmacological activity that are converted to the
active parent drug in vivo by enzymatic or chemical reactions or by a combination of the two …

Site-selective functionalization of hydroxyl groups in carbohydrate derivatives

V Dimakos, MS Taylor - Chemical reviews, 2018 - ACS Publications
Methods for site-selective transformations of hydroxyl groups in carbohydrate derivatives are
reviewed. The construction of oligosaccharides of defined connectivity hinges on such …

Ruthenium-catalyzed azide alkyne cycloaddition reaction: scope, mechanism, and applications

JR Johansson, T Beke-Somfai… - Chemical …, 2016 - ACS Publications
The ruthenium-catalyzed azide alkyne cycloaddition (RuAAC) affords 1, 5-disubstituted 1, 2,
3-triazoles in one step and complements the more established copper-catalyzed reaction …

Metabolism, biochemical actions, and chemical synthesis of anticancer nucleosides, nucleotides, and base analogs

J Shelton, X Lu, JA Hollenbaugh, JH Cho… - Chemical …, 2016 - ACS Publications
Nucleoside, nucleotide, and base analogs have been in the clinic for decades to treat both
viral pathogens and neoplasms. More than 20% of patients on anticancer chemotherapy …

The ProTide Prodrug Technology: From the Concept to the Clinic: Miniperspective

Y Mehellou, HS Rattan, J Balzarini - Journal of medicinal …, 2017 - ACS Publications
The ProTide technology is a prodrug approach developed for the efficient intracellular
delivery of nucleoside analogue monophosphates and monophosphonates. In this …

Prodrugs in medicinal chemistry and enzyme prodrug therapies

R Walther, J Rautio, AN Zelikin - Advanced drug delivery reviews, 2017 - Elsevier
Prodrugs are cunning derivatives of therapeutic agents designed to improve the
pharmacokinetics profile of the drug. Within a prodrug, pharmacological activity of the drug is …

Enantioselective hydrogen-bond-donor catalysis to access diverse stereogenic-at-P (V) compounds

KC Forbes, EN Jacobsen - Science, 2022 - science.org
The stereoselective synthesis of molecules bearing stereogenic phosphorus (V) centers
represents an enduring challenge in organic chemistry. Although stereospecific nucleophilic …

[HTML][HTML] Bulky P-stereogenic ligands. A success story in asymmetric catalysis

P Rojo, A Riera, X Verdaguer - Coordination Chemistry Reviews, 2023 - Elsevier
Since the development of BisP* ligand by Imamoto, P-stereogenic phosphines bearing a
bulky tert-butyl group and a smaller alkyl group have demonstrated extraordinary proficiency …

Catalytic asymmetric synthesis of the anti‐COVID‐19 drug remdesivir

M Wang, L Zhang, X Huo, Z Zhang… - Angewandte Chemie …, 2020 - Wiley Online Library
The catalytic asymmetric synthesis of the anti‐COVID‐19 drug Remdesivir has been
realized by the coupling of the P‐racemic phosphoryl chloride with protected nucleoside …

Bisphosphonates: The role of chemistry in understanding their biological actions and structure-activity relationships, and new directions for their therapeutic use

FH Ebetino, S Sun, P Cherian, S Roshandel… - Bone, 2022 - Elsevier
Abstract The bisphosphonates ((HO) 2 P (O) CR 1 R 2 P (O)(OH) 2, BPs) were first shown to
inhibit bone resorption in the 1960s, but it was not until 30 years later that a detailed …