Evidence map›Paper›PMID 37049777›Full record

ArticleMolecules (Basel, Switzerland)2023

Discovery of Novel EGFR Inhibitor Targeting Wild-Type and Mutant Forms of EGFR: In Silico and In Vitro Study.

Duangjai Todsaporn, Alexander Zubenko, Victor Kartsev, Thitinan Aiebchun, Panupong Mahalapbutr, Anthi Petrou, Athina Geronikaki, Liudmila Divaeva, Victoria Chekrisheva, Ilkay Yildiz and 2 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2023. 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
5.4field-weighted citation impact, top 4% 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

11 citing papers in PubMed, 21 citations in OpenAlex.

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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 8 institutions in 5 countries.

Duangjai TodsapornCenter of Excellence in Biocatalyst and Sustainable Biotechnology, Department of Biochemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
Alexander ZubenkoNorth-Caucasian Zonal Research Veterinary Institute, 346406 Novocherkassk, Russia.
Victor KartsevInterBioScreen Ltd., 85355 Moscow, Russia.
Thitinan AiebchunDepartment of Biochemistry, Faculty of Science, Kasetsart University, Bangkok 10900, Thailand.ORCID 0000-0001-8155-1602
Panupong MahalapbutrDepartment of Biochemistry, Faculty of Medicine, Khon Kaen University, Khon Kaen 40002, Thailand.ORCID 0000-0003-4389-334X
Anthi PetrouDepartment of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.ORCID 0000-0001-8587-2710
Athina GeronikakiDepartment of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.ORCID 0000-0001-9894-7777
Liudmila DivaevaInstitute of Physical and Organic Chemistry, Southern Federal University, Pr. Stachki 194/2, 344090 Rostov-on-Don, Russia.ORCID 0000-0002-7275-0797
Victoria ChekrishevaNorth-Caucasian Zonal Research Veterinary Institute, 346406 Novocherkassk, Russia.
Ilkay YildizSchool of Pharmacy, Ankara University, Ankara 06560, Turkey.ORCID 0000-0001-9526-0232
Kiattawee ChoowongkomonDepartment of Biochemistry, Faculty of Science, Kasetsart University, Bangkok 10900, Thailand.ORCID 0000-0002-2421-7859
Thanyada RungrotmongkolCenter of Excellence in Biocatalyst and Sustainable Biotechnology, Department of Biochemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
Aristotle University of Thessaloniki · GRChulalongkorn University · THKasetsart University · THNorth Caucasian Zonal Scientific Research Veterinary Institute · RUAnkara University · TRKhon Kaen University · THSouthern Federal University · RUTransgenomic (United States) · US

Funding

Fundamental Scientific Research of the State Academies of Sciences 0710-2019-0044Southern Federal University FENW-2023-0011Thailand Science research and Innovation Fund Chulalongkorn University HEA662300073
6 · The paper itself

Abstract

Targeting L858R/T790M and L858R/T790M/C797S mutant EGFR is a critical challenge in developing EGFR tyrosine kinase inhibitors to overcome drug resistance in non-small cell lung cancer (NSCLC). The discovery of next-generation EGFR tyrosine kinase inhibitors (TKIs) is therefore necessary. To this end, a series of furopyridine derivatives were evaluated for their EGFR-based inhibition and antiproliferative activities using computational and biological approaches. We found that several compounds derived from virtual screening based on a molecular docking and solvated interaction energy (SIE) method showed the potential to suppress wild-type and mutant EGFR. The most promising

Indexed as

Carcinoma, Non-Small-Cell LungLung NeoplasmsCell Line, TumorCell ProliferationDrug Resistance, NeoplasmErbB ReceptorsHumansMolecular Docking SimulationMutationProtein Kinase InhibitorsEGFR protein, humanErbB ReceptorsProtein Kinase Inhibitorscytotoxicitydrug screeningEGFR-TKfuropyridinemolecular dynamics

Identifiers

PMID37049777
PMCPMC10096398
OpenAlexW4361208043

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.