Evidence map›Paper›PMID 24315191›Full record

ArticleBioorganic & medicinal chemistry2014

Discovery of novel antitumor dibenzocyclooctatetraene derivatives and related biphenyls as potent inhibitors of NF-κB signaling pathway.

Fang-Lin Yu, Xiao-Yang He, Chunping Gu, Emika Ohkoshi, Li-Ting Wang, Sheng-Biao Wang, Chin-Yu Lai, Le Yu, Susan L Morris-Natschke, Kuo-Hsiung Lee and 2 more

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

Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.4field-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

1 citing paper in PubMed, 6 citations in OpenAlex.

  1. 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 3 institutions in 3 countries.

Fang-Lin YuBeijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
Xiao-Yang HeBeijing Institute of Pharmacology and Toxicology, Beijing 100850, China; Beijing Institute of Radiation Medicine, Beijing 100850, China.
Chunping GuSchool of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
Emika OhkoshiNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
Li-Ting WangNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
Sheng-Biao WangBeijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
Chin-Yu LaiNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
Le YuSchool of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.
Susan L Morris-NatschkeNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
Kuo-Hsiung LeeNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA; Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung, Taiwan. Electronic address: khlee@unc.edu.
Shuwen LiuSchool of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China. Electronic address: liusw@smu.edu.cn.
Lan XieBeijing Institute of Pharmacology and Toxicology, Beijing 100850, China. Electronic address: lanxieshi@yahoo.com.
University of North Carolina at Chapel Hill · USSouthern Medical University · CNBeijing Radiation Center · CN

Funding

Novel Antitumor AgentsR01CA177584 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, KUO-HSIUNG · 2013 to 2017
$1.9M
NCI NIH HHS CA177584NCI NIH HHS R01 CA177584
6 · The paper itself

Abstract

Several dibenzocyclooctatetraene derivatives (5-7) and related biphenyls (8-11) were designed, synthesized, and evaluated for inhibition of cancer cell growth and the NF-κB signaling pathway. Compound 5a, a dibenzocyclooctatetraene succinimide, was discovered as a potent inhibitor of the NF-κB signaling pathway with significant antitumor activity against several human tumor cell lines (GI₅₀ 1.38-1.45 μM) and was more potent than paclitaxel against the drug-resistant KBvin cell line. Compound 5a also inhibited LPS-induced NF-κB activation in RAW264.7 cells with an IC₅₀ value of 0.52 μM, prevented IκB-α degradation and p65 nuclear translocation, and suppressed LPS-induced NO production in a dose-dependent manner. The antitumor data in cellular assays indicated that relative positions and types of substituents on the dibenzocyclooctatetraene or acyclic biphenyl as well as torsional angles between the two phenyls are of primary importance to antitumor activity.

Indexed as

Anticarcinogenic AgentsBiological ProductsBiphenyl CompoundsHumansNF-kappa BSignal TransductionAnticarcinogenic AgentsBiological ProductsbiphenylBiphenyl CompoundsNF-kappa BAnticancer agentsDibenzocyclooctatetraene derivativesNF-κB inhibitorUnsymmetrical biphenyls

Identifiers

PMID24315191
PMCPMC3899348
OpenAlexW1998943282

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.