Synthesis of novel 1, 3, 4-oxadiazole derivatives as anti-esophageal cancer: In-vitro cytotoxic evaluation

In this work, an efficient protocol address a facile procedure employing safer and commercially available starting materials to afford the target products that are 1, 3, 4-oxadiazole derivatives (5a-c) in satisfactory yields with elevated purities. To elucidate these derivatives, their chemical structures were unambiguously confirmed by using different spectroscopic tools including FT-IR, NMR (1H and 13C), Mass spectra, and melting points. The enantiomers of the synthesized derivatives were checked by enantioselective HPLC analysis and NMR study which showed these derivatives obtained as racemates. With the aim to identify in vitro potency of these derivatives, MTT method has been applied to explore and evaluate their antiproliferative efficacy against esophageal cells (SKGT-4). The cell viability testing via MTT assay revealed that these derivatives displayed potent in vitro activity, showing IC50 values with a range of potential inhibition in comparison to the selected drug as a standard reference. The biological activity present in this work showed the synthesized derivatives offer significant antiproliferative efficacy with safer chemotherapeutic leads in medicinal chemistry to explorations for esophageal cancer treatment.

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Publication Details

Journal
Journal of Kufa for Chemical Sciences
Published
2025-06-20
DOI
https://doi.org/10.36329/jkcm/2025/v4.i2.16488
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.00

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article

Synthesis of novel 1, 3, 4-oxadiazole derivatives as anti-esophageal cancer: In-vitro cytotoxic evaluation

Ahmed Majeed Jassem, S. M. Hassan
Journal of Kufa for Chemical Sciences
Synthesis and biological activity
article

Synthesis of novel 1, 3, 4-oxadiazole derivatives as anti-esophageal cancer: In-vitro cytotoxic evaluation

Ahmed Majeed Jassem, S. M. Hassan
article en

Abstract

In this work, an efficient protocol address a facile procedure employing safer and commercially available starting materials to afford the target products that are 1, 3, 4-oxadiazole derivatives (5a-c) in satisfactory yields with elevated purities. To elucidate these derivatives, their chemical structures were unambiguously confirmed by using different spectroscopic tools including FT-IR, NMR (1H and 13C), Mass spectra, and melting points. The enantiomers of the synthesized derivatives were checked by enantioselective HPLC analysis and NMR study which showed these derivatives obtained as racemates. With the aim to identify in vitro potency of these derivatives, MTT method has been applied to explore and evaluate their antiproliferative efficacy against esophageal cells (SKGT-4). The cell viability testing via MTT assay revealed that these derivatives displayed potent in vitro activity, showing IC50 values with a range of potential inhibition in comparison to the selected drug as a standard reference. The biological activity present in this work showed the synthesized derivatives offer significant antiproliferative efficacy with safer chemotherapeutic leads in medicinal chemistry to explorations for esophageal cancer treatment.

Journal of Kufa for Chemical SciencesVol. 4(2)
University of Basrah (IQ)
University of Basrah
Openalex Percentile: Top 85%
Synthesis and biological activity
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Synthesis of novel 1, 3, 4-oxadiazole derivatives as anti-esophageal cancer: In-vitro cytotoxic evaluation — Ahmed Majeed Jassem, S. M. Hassan · Journal of Kufa for Chemical Sciences (2025) | TGRS Research Map | TGRS