Evidence map›Paper›PMID 39301897›Full record

ArticleAnti-cancer agents in medicinal chemistry2025

Synthesis of New Chromen-5-one Derivatives from Dimedone and their Antiproliferative Evaluations against Selected Cancer Cell Lines Together with Hepatocellular Carcinoma and Cervical Carcinoma.

Rafat Milad Mohareb, Mahmoud A Abdelaziz, Rasha Jame, Noha Omer, Hanan Maged Labib

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Article in Anti-cancer agents in medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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5 · Who and what money

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5 authors.

Rafat Milad MoharebDepartment of Chemistry, Faculty of Science, Cairo University, Giza, A. R. Egypt.ORCID 0000-0003-3922-803X
Mahmoud A AbdelazizDepartment of Chemistry, Faculty of Science, University of Tabuk, Tabuk, 71491, Kingdom of Saudi Arabia.
Rasha JameDepartment of Chemistry, Faculty of Science, University of Tabuk, Tabuk, 71491, Kingdom of Saudi Arabia.
Noha OmerDepartment of Chemistry, Faculty of Science, University of Tabuk, Tabuk, 71491, Kingdom of Saudi Arabia.
Hanan Maged LabibDepartment of chemistry, Faculty of Science, Cairo University, Giza, A. R. Egypt.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundThe coumarin nuclei, which exist in many heterocyclic compounds, has gained a lot of attention over the past decade due to their wide range of biological activities such as antibacterial, anticoagulant, antiviral, antifungal, anticancer, and anti-inflammatory properties.

objectiveThe multi-component reactions of 5,5-dimethylcyclohexane-1,3-dione with acetophenone derivatives and triethoxymethane produced biologically active target chromene molecules and their fused derivatives.

methodsThe reaction of 5,5-dimethylcyclohexane-1,3-dione and each of triethoxymethane and acetophenone derivatives 3a-g in absolute ethanol containing triethylamine gave the 4,6,7,8-tetrahydro-5H-chromen-5-one derivatives 4a-g. Compounds 4a-d were used for further heterocyclization reactions to produce biologically active fused pyrazole, thiophene, and thiazole derivative corporate with the chromenes caffold.

resultsThe cytotoxicity of the synthesized compounds were evaluated using six cancer cell lines together with c-Met kinase and PC-3 cell line inhibitions. In addition, cytotoxicity toward hepatocellular carcinoma HepG2 and cervical carcinoma HeLa was carried out as well as the in-vitro cytotoxic potential for all compounds against peripheral blood lymphocytes (PBL) extracted from healthy donors. Morphological changes of the A549 cell line by the two most active compounds were also studied.

conclusionThe synthesized heterocyclic compounds were originally obtained from 5,5-dimethylcyclohexane- 1,3-dione. Several of the produced compounds exhibited high inhibitions toward several cancer cell lines proving high inhibitions, therefore, encouraging further studies to synthesize heterocyclic compounds based on chromene scaffold.

Indexed as

Antineoplastic AgentsBenzopyransCarcinoma, HepatocellularChromonesLiver NeoplasmsUterine Cervical NeoplasmsCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorFemaleHumansMolecular StructureStructure-Activity RelationshipAntineoplastic AgentsBenzopyransChromones6-d]thiazolAntiproliferative activitychromen-5-oneChromeno[5coumarin nuclei.cytotoxicitymorphology

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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.