Evidence map›Paper›PMID 35741451›Full record

ArticleBiology2022

Identification of a Unique Cytotoxic Thieno[2,3-c]Pyrazole Derivative with Potent and Selective Anticancer Effects In Vitro.

Jessica D Hess, Luca H Macias, Denisse A Gutierrez, Karla Moran-Santibanez, Lisett Contreras, Stephanie Medina, Paulina J Villanueva, Robert A Kirken, Armando Varela-Ramirez, Manuel L Penichet and 1 more

Open access · goldAbstract read
In one paragraph

Article in Biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.4field-weighted citation impact, top 45% 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

6 citing papers in PubMed, 5 citations in OpenAlex.

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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

11 authors at 2 institutions in 1 country.

Jessica D HessDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.ORCID 0000-0001-8608-7458
Luca H MaciasDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.ORCID 0000-0003-2169-0322
Denisse A GutierrezDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.
Karla Moran-SantibanezDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.
Lisett ContrerasDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.
Stephanie MedinaDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.
Paulina J VillanuevaDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.ORCID 0000-0003-1195-2480
Robert A KirkenDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.
Armando Varela-RamirezDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.ORCID 0000-0002-2071-4874
Manuel L PenichetDivision of Surgical Oncology, Department of Surgery and Department of Microbiology, Immunology and Molecular Genetics, The Molecular Biology Institute, AIDS Institute, Jonsson Comprehensive Cancer Center, The University of California, Los Angeles, CA 90095, USA.
Renato J AguileraDepartment of Biological Sciences and Cellular Characterization and Biorepository Core Facility, Border Biomedical Research Center, The University of Texas at El Paso (UTEP), El Paso, TX 79902, USA.ORCID 0000-0003-3765-2793
The University of Texas at El Paso · USUniversity of California, Los Angeles · US

Funding

UTEP Border Biomedical Research CenterU54MD007592 · NIMHD · UNIVERSITY OF TEXAS EL PASO · PI ARSHAD M. KHAN · 2019 to 2026
$35.1M
RISE Scholars Program at UTEPR25GM069621 · NIGMS · UNIVERSITY OF TEXAS EL PASO · PI AGUILERA, RENATO J · 2004 to 2021
$11.2M
A Novel Strategy Targeting TfR1 for the Prevention/Treatment of AIDS-related NHLR01CA196266 · NCI · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI MARTINEZ-MAZA, OTONIEL, PENICHET, MANUEL L · 2016 to 2020
$3.4M
Characterization of novel compounds with anti-lymphoma activitySC3GM103713 · NIGMS · UNIVERSITY OF TEXAS EL PASO · PI AGUILERA, RENATO J · 2013 to 2016
$453k
NCI NIH HHS CA196266NCI NIH HHS R01 CA196266NIGMS NIH HHS 1SC3GM103713NIGMS NIH HHS R25 GM069621NIGMS NIH HHS R25GM069621NIGMS NIH HHS SC3 GM103713NIMHD NIH HHS 2U54MD007592NIMHD NIH HHS U54 MD007592
6 · The paper itself

Abstract

In recent years, the thienopyrazole moiety has emerged as a pharmacologically active scaffold with antitumoral and kinase inhibitory activity. In this study, high-throughput screening of 2000 small molecules obtained from the ChemBridge DIVERset library revealed a unique thieno[2,3-c]pyrazole derivative (Tpz-1) with potent and selective cytotoxic effects on cancer cells. Compound Tpz-1 consistently induced cell death at low micromolar concentrations (0.19 μM to 2.99 μM) against a panel of 17 human cancer cell lines after 24 h, 48 h, or 72 h of exposure. Furthermore, an in vitro investigation of Tpz-1's mechanism of action revealed that Tpz-1 interfered with cell cycle progression, reduced phosphorylation of p38, CREB, Akt, and STAT3 kinases, induced hyperphosphorylation of Fgr, Hck, and ERK 1/2 kinases, and disrupted microtubules and mitotic spindle formation. These findings support the continued exploration of Tpz-1 and other thieno[2,3-c]pyrazole-based compounds as potential small-molecule anticancer agents.

Indexed as

anticancer drug discoveryapoptosiscytotoxicitydifferential nuclear stainingkinase activity regulationleukemiamicrotubule disruptionmitotic spindle organizationthienopyrazole

Identifiers

PMID35741451
PMCPMC9219615
OpenAlexW4283073863

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.