Evidence map›Paper›PMID 31278031›Full record

ArticleBioorganic & medicinal chemistry letters2019

Styryl quinazolinones and its ethynyl derivatives induce myeloid differentiation.

Sridhar Radhakrishnan, Riyaz Syed, Hisashi Takei, Ikei S Kobayashi, Eugene Nakamura, Farheen Sultana, Ahmed Kamal, Daniel G Tenen, Susumu S Kobayashi

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. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.2field-weighted citation impact, top 52% 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

0 citing papers in PubMed, 2 citations in OpenAlex.

No citing paper in PubMed yet.

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 5 institutions in 4 countries.

Sridhar RadhakrishnanCancer Science Institute of Singapore, National University of Singapore, Singapore 117599, Singapore. Electronic address: csiradha@nus.edu.sg.
Riyaz SyedMedicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India; Department of Chemistry, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad 500 085, India.
Hisashi TakeiDepartment of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215, USA; Department of Medicine and Clinical Science, Gunma University Graduate School of Medicine, Maebashi, Gunma 371-8511, Japan.
Ikei S KobayashiDepartment of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215, USA.
Eugene NakamuraDepartment of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215, USA.
Farheen SultanaMedicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
Ahmed KamalMedicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India; School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi 110 062, India.
Daniel G TenenCancer Science Institute of Singapore, National University of Singapore, Singapore 117599, Singapore; Harvard Stem Cell Institute, Harvard Medical School, Boston, MA 02215, USA. Electronic address: daniel.tenen@nus.edu.sg.
Susumu S KobayashiDepartment of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215, USA; Division of Translational Genomics, Exploratory Oncology Research and Clinical Trial Center, National Cancer Center, Kashiwa, Chiba 277-8577, Japan. Electronic address: sukobaya@east.ncc.go.jp.
Harvard University · USIndian Institute of Chemical Technology · INBeth Israel Deaconess Medical Center · USChiba Cancer Center · JPNational University of Singapore · SG

Funding

Transcriptional and epigenetic heterogeneity of stem/progenitor cellsP01HL131477 · NHLBI · MASSACHUSETTS GENERAL HOSPITAL · PI DANIEL G TENEN · 2017 to 2026
$24.6M
Mechanisms of regulation by RNA in acute myeloid leukemiaR35CA197697 · NCI · BETH ISRAEL DEACONESS MEDICAL CENTER · PI TENEN, DANIEL G · 2015 to 2021
$7.1M
Overcoming resistance to tyrosine kinase inhibitors in lung cancerR01CA169259 · NCI · BETH ISRAEL DEACONESS MEDICAL CENTER · PI KOBAYASHI, SUSUMU · 2013 to 2018
$1.8M
Emergence of drug resistant mutations in lung cancerR21CA178301 · NCI · BETH ISRAEL DEACONESS MEDICAL CENTER · PI KOBAYASHI, SUSUMU · 2015 to 2016
$435k
NCCDPHP CDC HHS R01 DP000110NCI NIH HHS R01 CA169259NCI NIH HHS R21 CA178301NCI NIH HHS R35 CA197697NHLBI NIH HHS P01 HL131477
6 · The paper itself

Abstract

The tumor suppressor transcription factor CCAAT enhancer-binding protein α (C/EBPα) expression is downregulated in myeloid leukemias and enhancement of C/EBPα expression induces granulocytic differentiation in leukemic cells. Previously we reported that Styryl quinazolinones induce myeloid differentiation in HL-60 cells by upregulating C/EBPα expression. To identify more potent molecule that can induce leukemic cell differentiation we synthesized and evaluated new series of styryl quinazolinones, ethynyl styryl quinazolinones, styryl quinolinones and thienopyrimidinones. Thienopyrimidinones were found toxic and styryl quinolinones were found inactive. Ethynyl styryl quinazolinone 39 and styryl quinazolinone 5 were found active on par with the earlier reported analogues 1 and 2 suggesting that the 5-nitro furan-2-yl styryl quinazolinones find a real promise in leukemic cell differentiation. The improved potency of 5 suggested that further modifications in the 5-nitro furan-2-yl styryl quinazolinones can be at the phenyl substitution at the 3-position of the quinazolinone ring apart from the 5-position of the heteroaryl ring.

Indexed as

AlkynesAntineoplastic AgentsApoptosisCCAAT-Enhancer-Binding Protein-alphaCell DifferentiationCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHL-60 CellsHumansLeukemia, Myeloid, AcuteMolecular StructureQuinazolinonesStructure-Activity RelationshipAlkynesAntineoplastic AgentsCCAAT-Enhancer-Binding Protein-alphaQuinazolinonesApoptosisCCAAT/enhancer binding proteinMyeloid differentiationStyryl quinazolinonesThienopyrimidinone

Identifiers

PMID31278031
PMCPMC8236261
OpenAlexW2952866059

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.