Evidence map›Paper›PMID 28763643›Full record

ArticleEuropean journal of medicinal chemistry2017

Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers.

Dong-Jun Fu, Jian Song, Yu-Hui Hou, Ruo-Han Zhao, Jia-Huan Li, Ruo-Wang Mao, Jia-Jia Yang, Ping Li, Xiao-Lin Zi, Zhong-Hua Li and 5 more

Abstract read
In one paragraph

Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing 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

11 citing papers in PubMed.

  1. Review
  2. Review
  3. Current drug discovery technologies · 2024
    Review
  4. Article
  5. Review
  6. Review
  7. Article
  8. Article
  9. Essential Oil fromMolecules (Basel, Switzerland) · 2019
    Article
  10. Article
  11. 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

15 authors.

Dong-Jun FuNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Jian SongNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Yu-Hui HouNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Ruo-Han ZhaoNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Jia-Huan LiNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Ruo-Wang MaoNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Jia-Jia YangNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Ping LiNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Xiao-Lin ZiPathology and Laboratory Medicine, University of California, Irvine, Orange, CA 92868, USA.
Zhong-Hua LiNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Qing-Qing ZhangNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Fei-Yan WangNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China.
Sai-Yang ZhangSchool of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China. Electronic address: celeron16@163.com.
Yan-Bing ZhangNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China. Electronic address: zhangyb@zzu.edu.cn.
Hong-Min LiuNew Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, China; Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education, China; Key Laboratory of Henan Province for Drug Quality and Evaluation, China. Electronic address: liuhm@zzu.edu.cn.

Funding

The NEDD8 pathway mediated Skp2 degradation in chemoprevention by FKAR01CA193967 · NCI · UNIVERSITY OF CALIFORNIA-IRVINE · PI ZI, XIAOLIN · 2016 to 2020
$1.8M
NCI NIH HHS R01 CA193967
6 · The paper itself

Abstract

A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) for these 5,6-diaryl-1,2,4-triazines is explored in this report with evaluation of 15 variants of the structural class. Among these chemical derivatives, 3-(((1-(4-fluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)thio)-5,6-diphenyl-1,2,4-triazine (11E) showed the more potent inhibitory effect against three cell lines than 5-Fu. Cellular mechanism studies in MGC-803 cells elucidated 11E inhibited colony formation and arrested cell cycle at G2/M phase. Furthermore, compound 11E caused morphological changes, decreased mitochondrial membrane potential, and induced apoptosis through the apoptosis-related proteins in MGC-803 cells. It was the first time, to our knowledge, that 5,6-diaryl-1,2,4-triazines bearing a 1,2,3-triazole linker were used as potential apoptosis inducers.

Indexed as

Drug DiscoveryAntineoplastic AgentsApoptosisCell CycleCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMolecular StructureStructure-Activity RelationshipTriazines1,2,4-triazineAntineoplastic AgentsTriazines5,6-Diaryl-1,2,4-triazinesApoptosisApoptosis-related proteinsMolecular hybridization strategyMorphological changes

Identifiers

PMID28763643
PMCPMC5975277

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Registered trials

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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.