Evidence map›Paper›PMID 32957517›Full record

ArticleMolecules (Basel, Switzerland)2020

A Novel Cytotoxic Conjugate Derived from the Natural Product Podophyllotoxin as a Direct-Target Protein Dual Inhibitor.

Ángela-Patricia Hernández, Paula Díez, Pablo A García, Martín Pérez-Andrés, Pablo Ortega, Pablo G Jambrina, David Díez, María Ángeles Castro, Manuel Fuentes

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.5field-weighted citation impact, top 37% 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

4 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
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

9 authors at 2 institutions in 1 country.

Ángela-Patricia HernándezDepartamento de Ciencias Farmacéuticas, Área de Química Farmacéutica, Facultad de Farmacia, CIETUS/IBSAL, Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain.ORCID 0000-0002-5585-9918
Paula DíezDepartment of Medicine and General Cytometry Service-Nucleus, CIBERONC CB16/12/00400, Cancer Research Centre (IBMCC/CSIC/USAL/IBSAL), 37007 Salamanca, Spain.ORCID 0000-0003-2150-6898
Pablo A GarcíaDepartamento de Ciencias Farmacéuticas, Área de Química Farmacéutica, Facultad de Farmacia, CIETUS/IBSAL, Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain.ORCID 0000-0002-9060-577X
Martín Pérez-AndrésDepartment of Medicine and General Cytometry Service-Nucleus, CIBERONC CB16/12/00400, Cancer Research Centre (IBMCC/CSIC/USAL/IBSAL), 37007 Salamanca, Spain.
Pablo OrtegaDepartamento de Química Física, Facultad de Ciencias Químicas, Universidad de, 37008 Salamanca, Spain.ORCID 0000-0003-2480-6220
Pablo G JambrinaDepartamento de Química Física, Facultad de Ciencias Químicas, Universidad de, 37008 Salamanca, Spain.
David DíezDepartamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad de, 37008 Salamanca, Spain.ORCID 0000-0002-7261-8454
María Ángeles CastroDepartamento de Ciencias Farmacéuticas, Área de Química Farmacéutica, Facultad de Farmacia, CIETUS/IBSAL, Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain.ORCID 0000-0003-1638-4689
Manuel FuentesDepartment of Medicine and General Cytometry Service-Nucleus, CIBERONC CB16/12/00400, Cancer Research Centre (IBMCC/CSIC/USAL/IBSAL), 37007 Salamanca, Spain.ORCID 0000-0002-7305-3766
Universidad de Salamanca · ESInstituto de Investigación Biomédica de Salamanca · ES

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Natural products are the ideal basis for the design of novel efficient molecular entities. Podophyllotoxin, a naturally occurring cyclolignan, is an example of natural product which displays a high versatility from a biological activity point of view. Based on its unique chemical structure, different derivatives have been synthesized presenting the original antitumoral properties associated with the compound, i.e., the tubulin polymerization inhibition and arising anti-topoisomerase II activity from structural modifications on the cyclolignan skeleton. In this report, we present a novel conjugate or hybrid which chemically combines both biological activities in one single molecule. Chemical design has been planned based in our lead compound, podophyllic aldehyde, as an inhibitor of tubulin polymerization, and in etoposide, an approved antitumoral drug targeting topoisomerase II. The cytotoxicity and selectivity of the novel synthetized hybrid has been evaluated in several cell lines of different solid tumors. In addition, these dual functional effects of the novel compound have been also evaluated by molecular docking approaches.

Indexed as

AldehydesAntineoplastic Agents, PhytogenicApoptosisBiological ProductsCell Line, TumorDNA Topoisomerases, Type IIDrug Screening Assays, AntitumorEtoposideHumansMolecular Docking SimulationPodophyllotoxinStructure-Activity RelationshipTubulinTubulin ModulatorsAldehydesAntineoplastic Agents, PhytogenicBiological ProductsDNA Topoisomerases, Type IIEtoposidePodophyllotoxinTubulinTubulin Modulatorsanti-topoisomerase-IIconjugationcytotoxicityetoposideflow cytometryhybridizationmolecular dockingpodophyllotoxinprotein inhibitiontubulin polymerization

Identifiers

PMID32957517
PMCPMC7571232
OpenAlexW3086132942

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.