Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs.

doi:10.1016/j.bmcl.2011.05.009

Paper

Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs.

Published Jul 1, 2011 · Longqin Hu, Xinghua Wu, Jiye Han

Bioorganic & medicinal chemistry letters

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37

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1

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Abstract

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Study Snapshot

Nitrobenzyl phosphoramide mustards show potential as antiproliferative and antiparasitic agents, with 4-nitrobenzyl phosphoramide mustard offering the best combination of enzyme activity and antiproliferative effect against mammalian and trypanosomatid cells.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs.

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References

Exploiting the Drug-Activating Properties of a Novel Trypanosomal Nitroreductase

Halogenated nitrobenzylphosphoramide mustards represent a novel class of antitrypanosomal agents with potential for development of new therapeutics targeting a novel trypanosomal nitroreductase.

Design of anticancer prodrugs for reductive activation

Reductively activated anticancer prodrugs show promise in targeting tumor cells and reducing side effects, with potential for clinical use in cancer treatment.

Nitrofurantoin: the return of an old friend in the wake of growing resistance

Nitrofurantoin may be the best choice for treating uncomplicated urinary tract infections due to its low frequency of use and high susceptibility rate in common pathogens.

A mechanism for cross-resistance to nifurtimox and benznidazole in trypanosomes

Down-regulation of a key enzyme in trypanosomes can lead to resistance to nifurtimox and benznidazole, potentially impacting treatment for Chagas disease and African trypanosomiasis.

Tumour endoproteases: the cutting edge of cancer drug delivery?

Tumour endoprotease activated prodrugs show potential for improved cancer therapy by targeting tumor-specific enzymes and enhancing drug delivery to cancer cells.

Citations

In vitro anti‐trypanosomal activity of synthetic nitrofurantoin‐triazole hybrids against Trypanosoma species causing human African trypanosomosis

Nitrofurantoin-triazole hybrids show strong anti-trypanosomal activity against Trypanosoma species causing human African trypanosomosis, with potential as potential hit drugs.

In vitro evaluation of the selective cytotoxicity and genotoxicity of three synthetic ortho-nitrobenzyl derivatives in human cancer cell lines, with and without metabolic activation

Three synthetic ortho-nitrobenzyl derivatives show promising anticancer potential by selectively affecting cancer cell viability and causing chromosomal damage, especially after metabolic activation with the S9 fraction.

Dissecting the interstrand crosslink DNA repair system of Trypanosoma cruzi.

T. cruzi's DNA interstrand crosslink repair system can be targeted with inhibitors to enhance the potency of trypanocidal ICL-inducing compounds against Chagas disease.

An Update on African Trypanocide Pharmaceutics and Resistance

African trypanocide resistance is linked to mutations in key enzymes, making current treatments ineffective against various pathogens.

Synthesis and evaluation of new 4-peptidamido-2-fluorobenzyl phosphoramide mustard conjugates as prodrugs activated by prostate-specific antigen

Prodrugs with optimized substrates and linkers can achieve a balance between PSA cleavage rate and resistance to non-PSA-mediated hydrolysis, potentially benefiting prostate cancer treatment.