Evidence map›Paper›PMID 31383588›Full record

ArticleBioorganic & medicinal chemistry letters2019

Design, synthesis and anticancer activity of constrained sphingolipid-phenoxazine/phenothiazine hybrid constructs targeting protein phosphatase 2A.

Jean-Baptiste Garsi, Vito Vece, Lorenzo Sernissi, Catherine Auger-Morin, Stephen Hanessian, Alison N McCracken, Elizabeth Selwan, Cuauhtemoc Ramirez, Amogha Dahal, Nadine Ben Romdhane and 2 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2019. 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
0.3field-weighted citation impact, top 44% 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, 10 citations in OpenAlex.

  1. Article
  2. Review
  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

12 authors at 2 institutions in 2 countries.

Jean-Baptiste GarsiDepartment of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QC H3C 3J7, Canada.
Vito VeceDepartment of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QC H3C 3J7, Canada.
Lorenzo SernissiDepartment of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QC H3C 3J7, Canada.
Catherine Auger-MorinDepartment of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QC H3C 3J7, Canada.
Stephen HanessianDepartment of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QC H3C 3J7, Canada. Electronic address: stephen.hanessian@umontreal.ca.
Alison N McCrackenDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA.
Elizabeth SelwanDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA.
Cuauhtemoc RamirezDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA.
Amogha DahalDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA.
Nadine Ben RomdhaneDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA.
Brendan T FinicleDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA.
Aimee L EdingerDepartment of Developmental and Cell Biology, University of California, Irvine, 2128 Natural Sciences 1, CA 92697-2300, USA. Electronic address: aedinger@uci.edu.
University of California, Irvine · USUniversité de Montréal · CA

Funding

MINORITY BIOMEDICAL RESEARCHERS PROGRAMR25GM055246 · NIGMS · UNIVERSITY OF CALIFORNIA-IRVINE · PI MOTA-BRAVO, LUIS M · 1996 to 2022
$15.3M
CARCINOGENESIST32CA009054 · NCI · UNIVERSITY OF CALIFORNIA-IRVINE · PI EDINGER, AIMEE L, FRUMAN, DAVID ALEXANDER · 1985 to 2025
$8.6M
NCI NIH HHS T32 CA009054NIGMS NIH HHS R25 GM055246
6 · The paper itself

Abstract

Inspired by the cytotoxicity of perphenazine toward cancer cells and its ability to activate the serine/threonine protein phosphatase 2A (PP2A), we prepared series of ether-carbon linked analogs of a constrained synthetic sphingolipid analog 3, known for its cytotoxicity, nutrient transporter down-regulation and vacuolation properties, incorporating the tricyclic neuroleptics phenoxazine and phenothiazine to represent hybrid structures with possible synergistic cytotoxic activity. While the original activity of the lead compound 3 was diminished by fusion with the phenoxazine or phenothiazine tethered moieties, the corresponding 3-pyridyltetryl ether analog 10 showed cytotoxicity and nutrient transporter down-regulation similar to the lead compound 3, although it separated these PP2A-dependent phenotypes from that of vacuolation.

Indexed as

AnimalsAntineoplastic AgentsCell LineCell SurvivalDose-Response Relationship, DrugDrug DesignEnzyme InhibitorsMiceMolecular StructureOxazinesPhenothiazinesProtein Phosphatase 2SphingolipidsStructure-Activity RelationshipAntineoplastic AgentsEnzyme InhibitorsOxazinesphenothiazinePhenothiazinesphenoxazineProtein Phosphatase 2SphingolipidsCytotoxicity FL5.12Hybrid structuresNutrient transport down-regulationSphingolipidVacuolation

Identifiers

PMID31383588
PMCPMC7784717
OpenAlexW2963654051

What OpenQuestion holds

Textmetadata
LicenceTDM
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 OpenQuestion graph.