Results 31 to 40 of about 20,922 (255)

Dansyl linked solid phase resins as an educational tool to teach the concepts of high throughput screening and prodrugs.

open access: yesBritish Journal of Pharmacy, 2023
High throughput screening (HTS) and combinatorial chemistry, have been part of the process of drug design for nearly two decades. However, methods to teach their practical aspects to undergraduate students are scarce in the literature.
Jordi Morral   +3 more
doaj   +1 more source

Duocarmycin-based prodrugs for cancer prodrug monotherapy

open access: yesBioorganic & Medicinal Chemistry, 2008
The synthesis and biological evaluation of novel prodrugs based on the cytotoxic antibiotic duocarmycin SA (1) for a selective treatment of cancer using a prodrug monotherapy (PMT) are described. Transformation of the phenol 8 with the glucuronic acid benzyl ester trichloroacetimidate 9b followed by reaction with DMAI x HCl (10) gives the glucuronide ...
Tietze, Lutz Friedjan   +4 more
openaire   +3 more sources

Potential Development of Tumor-Targeted Oral Anti-Cancer Prodrugs: Amino Acid and Dipeptide Monoester Prodrugs of Gemcitabine

open access: yesMolecules, 2017
One of the main obstacles for cancer therapies is to deliver medicines effectively to target sites. Since stroma cells are developed around tumors, chemotherapeutic agents have to go through stroma cells in order to reach tumors.
Yasuhiro Tsume   +3 more
doaj   +1 more source

Investigating the crucial roles of aliphatic tails in disulfide bond-linked docetaxel prodrug nanoassemblies

open access: yesAsian Journal of Pharmaceutical Sciences, 2021
Disulfide bond-bridging strategy has been extensively utilized to construct tumor specificity-responsive aliphatic prodrug nanoparticles (PNPs) for precise cancer therapy.
Yuequan Wang   +10 more
doaj   +1 more source

Glucocorticoids-based prodrug design: Current strategies and research progress

open access: yesAsian Journal of Pharmaceutical Sciences
Attributing to their broad pharmacological effects encompassing anti-inflammation, antitoxin, and immunosuppression, glucocorticoids (GCs) are extensively utilized in the clinic for the treatment of diverse diseases such as lupus erythematosus, nephritis,
Hongbing Liu   +7 more
doaj   +1 more source

Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents

open access: yesArhiv za Higijenu Rada i Toksikologiju, 2020
Due to their very good chemical and proteolytic stability, ability to penetrate cell membranes, and resemblance to a peptide bond, carbamate derivatives have received much attention in recent years and got an important role in modern drug discovery and ...
Matošević Ana, Bosak Anita
doaj   +1 more source

Identifying transcription factors controlling the basal expression of human MRP4 highlights a substantial role for Sp1

open access: yesFEBS Open Bio, EarlyView.
The MRP4 transporter exports several drugs and signaling molecules. Here, we identified key promoter elements regulating basal MRP4 expression. Using reporter assays, we defined a conserved region with essential Sp1 and contributory Ets sites, which controlled basal MRP4 expression.
Debora Singer   +7 more
wiley   +1 more source

Optimizing the Pharmacological Properties of Discoidal Polymeric Nanoconstructs Against Triple-Negative Breast Cancer Cells

open access: yesFrontiers in Bioengineering and Biotechnology, 2020
Fine-tuning loading and release of therapeutic and imaging agents associated with polymeric matrices is a fundamental step in the preclinical development of novel nanomedicines. Here, 1,000 × 400 nm Discoidal Polymeric Nanoconstructs (DPNs) were realized
Miguel Ferreira   +9 more
doaj   +1 more source

UiO‐66 metal–organic frameworks in biomedicine: From structural tunability to bioimaging, photodiagnostics, and photodynamic cancer therapy

open access: yesFEBS Open Bio, EarlyView.
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová   +2 more
wiley   +1 more source

Recent progress in stimuli‐activable metallo‐prodrugs for cancer therapy

open access: yesSmart Molecules
The clinical approval of platinum‐based drugs has prompted the development of novel metallo‐complexes during the last several decades, while severe problems, especially for poor water solubility, drug resistance and toxicity in patients, greatly hindered
Jinzhe Liang, Fangmian Wei, Hui Chao
doaj   +1 more source

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