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ArticleCurrent medicinal chemistry2025

Organoselenium-based Azomethines as Apoptosis Inducers in Colorectal Carcinoma via P53, BAX, Caspase-3, Caspase-6, and Caspase-9 Modulations.

Saad Shaaban, Mohamed M Hammouda, Hanan A Althikrallah, Jawaher Y Al Nawah, Hussein Ba-Ghazal, Marwa Sharaky, Hamada S Abulkhair, Ahmed A Al-Karmalawy

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Article in Current medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

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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

2 citing papers in PubMed.

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4 · The record

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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

8 authors.

Saad ShaabanDepartment of Chemistry, College of Science, King Faisal University, Al-Ahsa, 31982, Saudi Arabia.
Mohamed M HammoudaDepartment of Chemistry, Faculty of Science, Mansoura University, 35516, Mansoura, Egypt.
Hanan A AlthikrallahDepartment of Chemistry, College of Science, King Faisal University, Al-Ahsa, 31982, Saudi Arabia.
Jawaher Y Al NawahDepartment of Chemistry, College of Science, King Faisal University, Al-Ahsa, 31982, Saudi Arabia.
Hussein Ba-GhazalDepartment of Chemistry, College of Science, King Faisal University, Al-Ahsa, 31982, Saudi Arabia.
Marwa SharakyCancer Biology Department, Pharmacology Unit, National Cancer Institute (NCI), Cairo University, Cairo, Egypt.
Hamada S AbulkhairPharmaceutical Organic Chemistry Department, Al-Azhar University, Nasr City, 11884, Cairo, Egypt.
Ahmed A Al-KarmalawyPharmaceutical Chemistry Department, Faculty of Pharmacy, Horus University-Egypt, New Damietta, 34518, Egypt.

Funding

Deputyship for Research and Innovation, Ministry of Education in Saudi Arabia INST211
6 · The paper itself

Abstract

backgroundOrganoselenium (OSe) agents and Schiff bases have demonstrated immense potential in the pharmaceutical field due to their broad spectrum of medicinal activities.

methodsWe herein report the antitumor activities of bis diselenide-based Schiff bases (3a-3c) derived from bis(4-aminophenyl)diselenide 2 and organoselenide-based Schiff bases (5a-c) derived from p-(methylselanyl)phenyl amine (4). The antitumor activity was estimated against fifteen cancer cell lines. Also, the growth inhibition percentage (GI%) of the Schiff bases tethered OSe compounds was evaluated against two normal cell lines, namely, human skin fibroblasts (HSF) and olfactory ensheathing cell line (OEC), to estimate the potential safety and selectivity. Furthermore, the cytotoxic inhibitory concentration 50 (IC50) was assessed against the cancer cell lines with the most outstanding GI% using the SRB assay.

resultsCompounds 3a, 3b, 3c, and 5a showed the lowest IC50 values compared to those of doxorubicin (DOX) against HCT116, HEPG2, A549, MDA-MB-468, and FaDu cancer cell lines, respectively, especially against the HCT116 subtype, assuring their potential anticancer activity. On the other side, the apoptotic potentials of the most active compounds (3a, 3b, 3c, and 5a) were also evaluated for apoptosis-related genes (P53, BAX, caspases 3, 6, 8, and 9, MMP2, MMP9, and BCL-2). Interestingly, compounds 3a, 3b, 3c, and 5a upregulated P53, BAX, and caspases 3, 6, 8, and 9 by (2.66, 2.26, 2.44, and 2.57)-, (1.62, 1.52, 1.37, and 1.47)-, (1.87, 1.75, 2.02, and 1.75)-, (1.96, 1.74, 2.06, and 2.30)-, (4.25, 3.78, 3.53, and 3.96)-, and (2.04, 1.72, 1.90, and 1.63)-fold change, respectively. Furthermore, MMP2, MMP9, and BCL-2 were downregulated by (0.39, 0.51, 0.33, and 0.28)-, (0.29, 0.32, 0.37, and 0.41)-, and (0.42, 0.35, 0.29, and 0.38)-fold-change, upon treatment with compounds 3a, 3b, 3c, and 5a, respectively, assuring the apoptotic potentials. Finally, molecular docking also greatly recommends the potential activity of the examined candidates (especially 3a and 3c) against the GSTP1 receptor as a recommended mechanism for their antitumor activity.

conclusionOur findings point to significant anticancer activities of Schiff bases tethered OSe agents, suggesting their promising potential for development as effective anticancer drugs.

Indexed as

Antineoplastic AgentsApoptosisColorectal NeoplasmsOrganoselenium CompoundsThiosemicarbazonesbcl-2-Associated X ProteinCaspase 3Caspase 9CaspasesCell Line, TumorCell ProliferationDrug Screening Assays, AntitumorHumansMolecular StructureSchiff BasesStructure-Activity RelationshipAntineoplastic AgentsBAX protein, humanbcl-2-Associated X ProteinCaspase 3Caspase 9CaspasesOrganoselenium CompoundsSchiff BasesThiosemicarbazonesTP53 protein, humanTumor Suppressor Protein p53anticancerapoptosiscolorectal carcinoma.cytotoxicityOrganoseleniumschiff bases

Identifiers

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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 Socratic graph.