Evidence map›Paper›PMID 32963943›Full record

ArticleActa pharmaceutica Sinica. B2020

Design, synthesis and pharmacological evaluation of 4-(3-chloro-4-(3-cyclopropylthioureido)-2-fluorophenoxy)-7-methoxyquinoline-6-carboxamide (WXFL-152): a novel triple angiokinase inhibitor for cancer therapy.

Yuqin Yao, Zhuowei Liu, Manyu Zhao, Zhengxia Chen, Peng Li, Yang Zhang, Yuxi Wang, Chengjian Zhao, Chaofeng Long, Xiaoxin Chen and 1 more

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

Article in Acta pharmaceutica Sinica. B, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.4field-weighted citation impact, top 19% 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

7 citing papers in PubMed, 20 citations in OpenAlex.

  1. 7-azaindole as privileged scaffold: Advances in drug design and structural modification.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
    Review
  2. Review
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  4. Angiogenic signaling pathways and anti-angiogenic therapy for cancer.Signal transduction and targeted therapy · 2023
    Review
  5. Article
  6. Targeting fibrosis, mechanisms and cilinical trials.Signal transduction and targeted therapy · 2022
    Review
  7. 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

11 authors at 4 institutions in 1 country.

Yuqin YaoState Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.
Zhuowei LiuState Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.
Manyu ZhaoState Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.
Zhengxia ChenWuXi AppTec Ltd. Shanghai 200131, China.
Peng LiWuXi AppTec Ltd. Shanghai 200131, China.
Yang ZhangWuXi AppTec Ltd. Shanghai 200131, China.
Yuxi WangState Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.
Chengjian ZhaoState Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.
Chaofeng LongGuangdong Zhongsheng Pharmaceutical Co., Ltd., Dongguan 523325, China.
Xiaoxin ChenGuangdong Zhongsheng Pharmaceutical Co., Ltd., Dongguan 523325, China.
Jinliang YangState Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.
Sichuan University · CNWuXi AppTec (China) · CNGuangdong Pharmaceutical University · CNState Key Laboratory of Biotherapy

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Angiokinases, such as vascular endothelial-, fibroblast- and platelet-derived growth factor receptors (VEGFRs, FGFRs and PDGFRs) play crucial roles in tumor angiogenesis. Anti-angiogenesis therapy using multi-angiokinase inhibitor has achieved great success in recent years. In this study, we presented the design, synthesis, target identification, molecular mechanism, pharmacodynamics (PD) and pharmacokinetics (PK) research of a novel triple-angiokinase inhibitor WXFL-152. WXFL-152, identified from a series of 4-oxyquinoline derivatives based on a structure-activity relationship study, inhibited the proliferation of vascular endothelial cells (ECs) and pericytes by blocking the angiokinase signals VEGF/VEGFR2, FGF/FGFRs and PDGF/PDGFR

Indexed as

Anti-angiogenesis therapyATCC, American Type Culture CollectionAUC, area under the plasma concentration–time curveCE, collision energyCL, systemic clearanceCmax, maximum plasma concentrationDrug synthesisECM, endothelial cell mediumEC, vascular endothelial cellERKs, extracellular signal-regulated kinasesFGF, fibroblast growth factorFGFRs, fibroblast growth factor receptorsHBVPs, human brain vascular pericytesHUVECs, human umbilical vein endothelial cellsIC50, half maximal inhibitory concentrationIHC, immunohistochemistryi.v., intravenous injectionLC–MS, liquid chromatography mass spectrometryLLOQ, lower limit of quantificationMRM, multiple reaction monitoringMsOH, methane sulfonic acidMulti-angiokinase inhibitorNMR, nuclear magnetic resonancePDB, protein data bankPDGF, platelet-derived growth factorPDGFRs, platelet-derived growth factor receptorsPD, pharmacodynamicsPDX, patient-derived tumor xenograftPharmacokineticPK, pharmacokineticsPM, pericyte mediump.o., per osQC, quality controlRE, values and relative errorRSD, relative standard deviationRTKs, receptor tyrosine kinasesTGI, tumor growth inhibition rateTLC, thin-layer chromatographyTmax, time the maximum concentration occurredTumorULOQ, up limit of quantitationVdss, volume of distribution at steady stateVEGFRs, vascular endothelial growth factor receptorsVEGF, vascular endothelial growth factor

Identifiers

PMID32963943
PMCPMC7488503
OpenAlexW3017329568

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.