ArticleNucleic acids research2014
Conjugation with polyamines enhances the antibacterial and anticancer activity of chloramphenicol.
Article in Nucleic acids research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
17 citing papers in PubMed, 42 citations in OpenAlex.
- Cationic Polymers Enable Internalization of Negatively Charged Chemical Probes into Bacteria.ACS chemical biology · 2023Article
- Development of Responsive Nanoparticles for Cancer Therapy.International journal of molecular sciences · 2023Article
- Polyamine-Drug Conjugates: Do They Boost Drug Activity?Molecules (Basel, Switzerland) · 2023Review
- Chloramphenicol Derivatization in Its Primary Hydroxyl Group with Basic Amino Acids Leads to New Pharmacophores with High Antimicrobial Activity.Antibiotics (Basel, Switzerland) · 2023Article
- Electroresponsive and pH-Sensitive Hydrogel as Carrier for Controlled Chloramphenicol Release.Biomacromolecules · 2023Article
- Conjugates of Chloramphenicol Amine and Berberine as Antimicrobial Agents.Antibiotics (Basel, Switzerland) · 2022Article
- Exploring the Diversity and Antibacterial Potentiality of Cultivable Actinobacteria from the Soil of the Saxaul Forest in Southern Gobi Desert in Mongolia.Microorganisms · 2022Article
- Triphenilphosphonium Analogs of Chloramphenicol as Dual-Acting Antimicrobial and Antiproliferating Agents.Antibiotics (Basel, Switzerland) · 2021Article
- Binding and Action of Triphenylphosphonium Analog of Chloramphenicol upon the Bacterial Ribosome.Antibiotics (Basel, Switzerland) · 2021Article
- Recent Trends in Synthesis of Chloramphenicol New Derivatives.Antibiotics (Basel, Switzerland) · 2021Article
- Incorporation of Chloramphenicol Loaded Hydroxyapatite Nanoparticles into Polylactide.International journal of molecular sciences · 2019Article
- New Chloramphenicol Derivatives from the Viewpoint of Anticancer and Antimicrobial Activity.Antibiotics (Basel, Switzerland) · 2019Article
- The Aromatic Head Group of Spider Toxin Polyamines Influences Toxicity to Cancer Cells.Toxins · 2017Article
- Ground-state dioxygen undergoes metal-free [3 + 2]-annulations with allenes and nitrosoarenes under ambient conditions.Chemical science · 2017Article
- The antibiotic chloramphenicol may be an effective new agent for inhibiting the growth of multiple myeloma.Oncotarget · 2016Article
- Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions.Antibiotics (Basel, Switzerland) · 2016Review
- Synthesis and evaluation of chloramphenicol homodimers: molecular target, antimicrobial activity, and toxicity against human cells.PloS one · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chloramphenicol (CAM) is a broad-spectrum antibiotic, limited to occasional only use in developed countries because of its potential toxicity. To explore the influence of polyamines on the uptake and activity of CAM into cells, a series of polyamine-CAM conjugates were synthesized. Both polyamine architecture and the position of CAM-scaffold substitution were crucial in augmenting the antibacterial and anticancer potency of the synthesized conjugates. Compounds 4 and 5, prepared by replacement of dichloro-acetyl group of CAM with succinic acid attached to N4 and N1 positions of N(8),N(8)-dibenzylspermidine, respectively, exhibited higher activity than CAM in inhibiting the puromycin reaction in a bacterial cell-free system. Kinetic and footprinting analysis revealed that whereas the CAM-scaffold preserved its role in competing with the binding of aminoacyl-tRNA 3'-terminus to ribosomal A-site, the polyamine-tail could interfere with the rotatory motion of aminoacyl-tRNA 3'-terminus toward the P-site. Compared to CAM, compounds 4 and 5 exhibited comparable or improved antibacterial activity, particularly against CAM-resistant strains. Compound 4 also possessed enhanced toxicity against human cancer cells, and lower toxicity against healthy human cells. Thus, the designed conjugates proved to be suitable tools in investigating the ribosomal catalytic center plasticity and some of them exhibited greater efficacy than CAM itself.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.