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Reversing the undesirable pH-profile of doxorubicin via activation of a di-substituted maleamic acid prodrug at tumor acidity.
- Source :
-
Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2017 Nov 28; Vol. 53 (95), pp. 12826-12829. - Publication Year :
- 2017
-
Abstract
- The acid-labile behavior of di-substituted maleamic acid (DMA) and its equilibrium with di-substituted maleimide (DMI) are exploited to build an ultra acid-sensitive, small molecule prodrug that can be activated by tumor extracellular pH (pHe) in the range of 6.5-6.9. Such a DMA prodrug reversed the unfavorable pH-profile of doxorubicin (Dox), which may improve its therapeutic window.
- Subjects :
- Antibiotics, Antineoplastic administration & dosage
Antibiotics, Antineoplastic chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Cell Survival drug effects
Dose-Response Relationship, Drug
Doxorubicin administration & dosage
Doxorubicin chemistry
Drug Screening Assays, Antitumor
Humans
Hydrogen-Ion Concentration
Maleates chemical synthesis
Maleates chemistry
Maleimides chemistry
Molecular Structure
Prodrugs chemical synthesis
Prodrugs chemistry
Structure-Activity Relationship
Antibiotics, Antineoplastic pharmacology
Doxorubicin pharmacology
Maleates pharmacology
Maleimides pharmacology
Prodrugs pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1364-548X
- Volume :
- 53
- Issue :
- 95
- Database :
- MEDLINE
- Journal :
- Chemical communications (Cambridge, England)
- Publication Type :
- Academic Journal
- Accession number :
- 29143021
- Full Text :
- https://doi.org/10.1039/c7cc06843c