Evidence map›Paper›PMID 38138441›Full record

ArticleMolecules (Basel, Switzerland)2023

Synthesis and Antiproliferative Potential of Thiazole and 4-Thiazolidinone Containing Motifs as Dual Inhibitors of EGFR and BRAF

Alaa A Hassan, Nasr K Mohamed, Ashraf A Aly, Mohamed Ramadan, Hesham A M Gomaa, Ahmed T Abdel-Aziz, Bahaa G M Youssif, Stefan Bräse, Olaf Fuhr

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 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.6field-weighted citation impact, top 36% 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

4 citing papers in PubMed, 4 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

9 authors at 5 institutions in 3 countries.

Alaa A HassanChemistry Department, Faculty of Science, Organic Division, Minia University, Minia 61519, Egypt.
Nasr K MohamedChemistry Department, Faculty of Science, Organic Division, Minia University, Minia 61519, Egypt.
Ashraf A AlyChemistry Department, Faculty of Science, Organic Division, Minia University, Minia 61519, Egypt.ORCID 0000-0002-0314-3408
Mohamed RamadanPharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt.ORCID 0000-0002-7975-3421
Hesham A M GomaaDepartment of Pharmacology, College of Pharmacy, Jouf University, Sakaka 72341, Aljouf, Saudi Arabia.ORCID 0000-0001-7510-8428
Ahmed T Abdel-AzizChemistry Department, Faculty of Science, Organic Division, Minia University, Minia 61519, Egypt.
Bahaa G M YoussifPharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.ORCID 0000-0002-6834-6548
Stefan BräseInstitute of Organic Chemistry, Karlsruher Institut fur Technologie, 76131 Karlsruhe, Germany.ORCID 0000-0003-4845-3191
Olaf FuhrInstitute Karlsruhe of Nanotechnology (INT) and Karlsruhe Nano Micro Facility (KNMFi), Institute of Technology (KIT), 76344 Eggenstein-Leopoldshafen, Germany.ORCID 0000-0003-3516-2440
Minia University · EGKarlsruhe Institute of Technology · DEAl-Azhar University · EGAssiut University · EGJouf University · SA

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Thiazole and thiazolidinone recur in a wide range of biologically active compounds that reach different targets within the context of tumors and represent a promising starting point to access potential candidates for treating metastatic cancer. Therefore, searching for new lead compounds that show the highest anticancer potency with the fewest adverse effects is a major drug-discovery challenge. Because the thiazole ring is present in dasatinib, which is currently used in anticancer therapy, it is important to highlight the ring. In this study, cycloalkylidenehydrazinecarbothioamides (cyclopentyl, cyclohexyl, cyclooctyl, dihydronapthalenylidene, flurine-9-ylidene, and indolinonyl) reacted with 2-bromoacetophenone and diethylacetylenedicarboxylate to yield thiazole and 4-thiazolidinone derivatives. The structure of the products was confirmed by using infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry, and single-crystal X-ray analyses. The antiproliferative activity of the newly synthesized compounds was evaluated. The most effective inhibitory compounds were further tested in vitro against both epidermal growth factor receptor (EGFR) and B-Raf proto-oncogene, serine/threonine kinase (BRAF

Indexed as

Antineoplastic AgentsThiazolesCell Line, TumorCell ProliferationDrug Screening Assays, AntitumorErbB ReceptorsHumansMolecular Docking SimulationNeoplasm Recurrence, LocalProtein Kinase InhibitorsProto-Oncogene Proteins B-rafThiazolidines4-thiazolidinoneAntineoplastic AgentsBRAF protein, humanEGFR protein, humanErbB ReceptorsProtein Kinase InhibitorsProto-Oncogene Proteins B-rafThiazolesThiazolidines4-thiazolidinoneanticancerBRAFdual inhibitorsEGFRthiazole

Identifiers

PMID38138441
PMCPMC10745574
OpenAlexW4389348558

What OpenQuestion holds

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LicenceCC BY
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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.