Evaluation Of Ethyl 4-(Chlorophenyl Amino)-5 Methyl Thieno[2,3-D] Pyrimidine-6-Carboxylate for Its Anticancer Activity Focusing on EGFR Inhibition

Thienopyrimidines can be regarded as a potential candidate for the treatment of cancer. In this study Ethyl 4-(chlorophenyl amino)-5 methyl thieno[2,3-d]pyrimidine-6-carboxylate; named as AV79 is evaluated for its anticancer potential . The compound is a thienopyrimidine derivative and this skeletal structure has been extensively studied for its EGFR inhibiting property. The amino and ester substitutions on the basic ring structure will enhance its chemotherapeutic activity. The compound is subjected to docking studies to find out the drug-target interaction. The objective of the study is to understand the molecular mechanism by which this chemical analog carry out is activity. MTT assay and neutral red assay are done to get a clear idea about its cytotoxic potential. Apoptosis assay by acridine orange and ethidium bromide double staining was done to determine the mechanism of cell death caused by the compound. Transwell migration assay is performed to detect whether this chemical analog could inhibit the migration of tumor cells. TMRE and DAPI staining is done to detect the cell death caused by AV79. Comet assay is also done to evaluate the genotoxicity.

Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2024-12-20
DOI
https://doi.org/10.5281/zenodo.14535564
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
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article

Evaluation Of Ethyl 4-(Chlorophenyl Amino)-5 Methyl Thieno[2,3-D] Pyrimidine-6-Carboxylate for Its Anticancer Activity Focusing on EGFR Inhibition

Zenodo (CERN European Organization for Nuclear Research)
Synthesis and biological activity
article

Evaluation Of Ethyl 4-(Chlorophenyl Amino)-5 Methyl Thieno[2,3-D] Pyrimidine-6-Carboxylate for Its Anticancer Activity Focusing on EGFR Inhibition

article en

Abstract

Thienopyrimidines can be regarded as a potential candidate for the treatment of cancer. In this study Ethyl 4-(chlorophenyl amino)-5 methyl thieno[2,3-d]pyrimidine-6-carboxylate; named as AV79 is evaluated for its anticancer potential . The compound is a thienopyrimidine derivative and this skeletal structure has been extensively studied for its EGFR inhibiting property. The amino and ester substitutions on the basic ring structure will enhance its chemotherapeutic activity. The compound is subjected to docking studies to find out the drug-target interaction. The objective of the study is to understand the molecular mechanism by which this chemical analog carry out is activity. MTT assay and neutral red assay are done to get a clear idea about its cytotoxic potential. Apoptosis assay by acridine orange and ethidium bromide double staining was done to determine the mechanism of cell death caused by the compound. Transwell migration assay is performed to detect whether this chemical analog could inhibit the migration of tumor cells. TMRE and DAPI staining is done to detect the cell death caused by AV79. Comet assay is also done to evaluate the genotoxicity.

Zenodo (CERN European Organization for Nuclear Research)
Good health and well-being
Openalex Percentile: Top 62%
Synthesis and biological activity
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