Evidence map›Paper›PMID 27082930›Full record

ArticleACS combinatorial science2016

Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach.

Jinbao Xiang, Zhuoqi Zhang, Yan Mu, Xianxiu Xu, Sigen Guo, Yongjin Liu, Daniel P Russo, Hao Zhu, Bing Yan, Xu Bai

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS combinatorial science, 2016. 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
–field-weighted citation impact
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.

  1. Discovery of a 6-Aminobenzo[ACS pharmacology & translational science · 2024
    Article
  2. Ultrasound for Drug Synthesis: A Green Approach.Pharmaceuticals (Basel, Switzerland) · 2020
    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

10 authors.

Jinbao XiangThe Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, and The College of Chemistry, Jilin University , Changchun, Jilin 130021, P. R. China.
Zhuoqi ZhangThe Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, and The College of Chemistry, Jilin University , Changchun, Jilin 130021, P. R. China.
Yan MuSchool of Chemistry and Chemical Engineering, Shandong University , Jinan, Shandong 250100, P. R. China.
Xianxiu XuThe Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, and The College of Chemistry, Jilin University , Changchun, Jilin 130021, P. R. China.
Sigen GuoThe Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, and The College of Chemistry, Jilin University , Changchun, Jilin 130021, P. R. China.
Yongjin LiuSchool of Chemistry and Chemical Engineering, Shandong University , Jinan, Shandong 250100, P. R. China.
Daniel P RussoThe Rutgers Center for Computational and Integrative Biology , Camden, New Jersey 08102, United States.
Hao ZhuThe Rutgers Center for Computational and Integrative Biology , Camden, New Jersey 08102, United States.
Bing YanSchool of Chemistry and Chemical Engineering, Shandong University , Jinan, Shandong 250100, P. R. China.
Xu BaiThe Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, and The College of Chemistry, Jilin University , Changchun, Jilin 130021, P. R. China.

Funding

Translational Research Support CoreP30ES005022 · NIEHS · UNIV OF MED/DENT NJ-R W JOHNSON MED SCH · PI ROBERT John LAUMBACH · 1988 to 2026
$47.4M
Predictive Computational Acute Toxicity Modeling by Profiling Chemicals With PublR15ES023148 · NIEHS · RUTGERS THE STATE UNIV OF NJ CAMDEN · PI ZHU, HAO · 2013 to 2018
$941k
NIEHS NIH HHS P30 ES005022NIEHS NIH HHS R15 ES023148
6 · The paper itself

Abstract

An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 μM), which exhibits much less toxicity toward normal cells (EC50 > 100 μM against normal human fibroblasts). The most active hits also exhibited drug-like properties suitable for further preclinical research. This redeployment of antidepressing compounds for anticancer applications provides promising future prospects for treating drug-resistant tumors with fewer side effects.

Indexed as

Antineoplastic AgentsCell Line, TumorCells, CulturedDrug DiscoveryDrug Resistance, NeoplasmHumansThiazepinesAntineoplastic AgentsThiazepinesantidepressingH460TaxRredeploymentselective cytotoxicitytricyclic thiazepine

Identifiers

PMID27082930
PMCPMC5592639

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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.