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Prodrugs
Prodrugs are a widely deployed strategy for medical chemists. Introduction of the prodrug typically moderates the physicochemical properties of the... -
Synthesis, characterization and pharmacological screening of etodolac amino acid’s mutual prodrugs
Etodolac is the drug of choice for pain and inflammation associated with rheumatoid arthritis. Here, the mutual prodrugs of etodolac were synthesized...
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Synthesis of Pregnane–Cholesterol and Cholesterol–Cholesterol Prodrugs via Ring A–Ring A Connection. Potential Cytotoxic Activity against Cervical Cancer Cell Line HeLa
AbstractTwo novel pregnane–cholesterol and cholesterol–cholesterol prodrugs have been synthesized. The synthetic route involved preparation of...
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Pt(IV) Complexes in the Search for Novel Platinum Prodrugs with Promising Activity
The kinetically inert, six coordinated, octahedral Pt(IV) complexes are termed dual-, triple-, or multi-action prodrugs based on the nature of the...
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Dual Diomarkers Triggered Prodrugs for Precise Treatment of Melanoma: Design, Synthesis and Activities
Targeted prodrug strategy, which utilizes the endogenous biomarkers in cancer cells as activators to release the active drug, has been well...
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Radiotherapy activates picolinium prodrugs in tumours
Radiotherapy-induced prodrug activation provides an ideal solution to reduce the systemic toxicity of chemotherapy in cancer therapy, but the scope...
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Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
A widely established prodrug strategy can effectively optimize the unappealing properties of therapeutic agents in cancer treatment. Among them,...
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First- and Second-Generation Nucleoside Triphosphate Prodrugs: TriPPPro-Compounds for Antiviral Chemotherapy
Currently, a number of biologically active nucleoside analogues are extensively used as antiviral, anticancer, antiparasitic, and antibacterial... -
Switching on prodrugs using radiotherapy
Chemotherapy is a powerful tool in the armoury against cancer, but it is fraught with problems due to its global systemic toxicity. Here we report...
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First and Second Generation Nucleoside Triphosphate Prodrugs: TriPPPro-Compounds for Antiviral Chemotherapy
Currently, a number of biologically active nucleoside analogues are extensively used as antiviral, anticancer, antiparasitic, and antibacterial... -
Design Principles and Development of Prodrugs for Multiply Active Antibacterials
Added layers of complexity in design are inherent with multi-action agents released from prodrugs, and though challenging, such prodrugs do offer... -
New acetylenic derivatives of bile acids as versatile precursors for the preparation of prodrugs. Synthesis and cytotoxicity study
Three groups of bile acid derivatives with acetylenic moieties, such as propargyl, hex-5-ynoyl, and 4,7,10,13-tetraoxahexadec-15-ynoyl ones, were...
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Synthesis of diosgenin prodrugs: anti-inflammatory and antiproliferative activity evaluation
AbstractIn this work, we evaluated the antiproliferative and anti-inflammatory activities of two diosgenin prodrugs. The prodrugs were obtained by...
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Domino Dendrimers
Domino dendrimers have recently been developed and introduced as a potential platform for a single triggered multi-prodrug. Surprisingly, three... -
Hydrogen-bonded organic framework-based bioorthogonal catalysis prevents drug metabolic inactivation
Bioorthogonal chemistry provides a new avenue for disease treatment by generating therapeutic agents in situ. However, two crucial issues have to be...
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DSC studies on the interaction of lipophilic cytarabine prodrugs with DMPC multilamellar vesicles
Cytarabine (1-β- d -arabinofuranosylcytosine, Ara-C), a pyrimidine nucleoside analogue, is used for the treatment of both acute and chronic...
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Correction: Cyclopeptidic photosensitizer prodrugs as proteolytically triggered drug delivery systems of pheophorbide A: part I – self-quenched prodrugs
The authors regret a spelling mistake in the surname of one of the authors. The surname given as Yuschenko should be Yushchenko. The correct spelling...
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A3 Adenosine Receptor Ligands: From Discovery to Clinical Trials
Numerous classes of selective agonists, antagonists, and allosteric modulators of the A3 adenosine receptor (AR) have been reported. The... -
Cross-linked lipoic acid nanocapsules serve as H2O2 amplifier to strengthen the H2O2-sensitive prodrug activation
The H 2 O 2 -triggered prodrug activation represents a hot topic while the low H 2 O 2 level of cancer cells hindered the complete activation of parent...
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Amino acid tethered benzoxazolone as highly potent inhibitors of O-glycosylation
Novel inhibitors of GlcNAc-Ts have been reported based on benzoxazolone appended amino acids/esters which showed a competitive inhibition of the...