Evidence map›Paper›PMID 32462253›Full record

ArticlePharmaceutical research2020

Synthesis and Evaluation of Antitumor Alkylphospholipid Prodrugs.

Boris Gaillard, Jean-Serge Remy, Françoise Pons, Luc Lebeau

Open access · greenAbstract read
PubMed Publisher
In one paragraph

Article in Pharmaceutical research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.1field-weighted citation impact, top 42% of its field
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

4 authors at 1 institution in 1 country.

Boris GaillardLaboratoire de Conception et Application de Molécules Bioactives, UMR 7199 CNRS - Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin - BP 60024, 67401, Illkirch, France.
Jean-Serge RemyLaboratoire de Conception et Application de Molécules Bioactives, UMR 7199 CNRS - Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin - BP 60024, 67401, Illkirch, France.
Françoise PonsLaboratoire de Conception et Application de Molécules Bioactives, UMR 7199 CNRS - Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin - BP 60024, 67401, Illkirch, France.
Luc LebeauLaboratoire de Conception et Application de Molécules Bioactives, UMR 7199 CNRS - Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin - BP 60024, 67401, Illkirch, France. llebeau@unistra.fr.ORCID http://orcid.org/0000-0002-3276-6727
Centre National de la Recherche Scientifique · FR

Funding

Alsace contre le cancer 2015Conseil Régional d'Alsace 2015LabEx Medalis 2015
6 · The paper itself

Abstract

purposeHemolysis is a serious side effect of antitumor alkylphospholipids (APLs) that limits dose levels and is a constraint in their use in therapeutic regimen. Nine prodrugs of promising APLs (miltefosine, perifosine, and erufosine) were synthesized so as to decrease their membrane activity and improve their toxicity profile while preserving their antineoplastic potency.

methodsThe synthesis of the pro-APLs was straightforwardly achieved in one step starting from the parent APLs. The critical aggregation concentration of the prodrugs, their hydrolytic stability under various pH conditions, their blood compatibility and cytotoxicity in three different cell lines were determined and compared to those of the parent antitumor lipids.

resultsThe APL prodrugs display antitumor activity which is similar to that of the parent alkylphospholipids but without associated hemolytic toxicity.

conclusionThe pro-APL compounds may be considered as intravenously injectable derivatives of APLs. They could thus address one of the major issues met in cancer therapies involving antitumor lipids and restricting their utilization to oral and topical administration because of limited maximum tolerated dose.

Indexed as

Administration, IntravenousAntineoplastic AgentsCell Line, TumorDrug Screening Assays, AntitumorDrug StabilityHemolysisHumansMaximum Tolerated DoseNeoplasmsOrganophosphatesPhosphorylcholineProdrugsQuaternary Ammonium CompoundsAntineoplastic Agentserucylphospho-N,N,N-trimethylpropylammoniummiltefosineOrganophosphatesperifosinePhosphorylcholineProdrugsQuaternary Ammonium Compoundsalkylphospholipiderufosinehemolytic toxicitymiltefosineperifosineprodrug

Identifiers

PMID32462253
OpenAlexW3030388463

What Socratic holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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 Socratic graph.