Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects

Objective: Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. Methods: In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. Results and Discussion: Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (VI), (VII), (VIII), (IX), and (XII) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (VII) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (VI–IX), and (XII), just and just, 2-F derivative (IV) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. Conclusions: The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.

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Journal
Russian Journal of Bioorganic Chemistry
Published
2024-12-01
DOI
https://doi.org/10.1134/s1068162024060062
Primary Topic
Synthesis and biological activity
Type
article
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article

Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects

Leila Hosseinzadeh, Hossein Malekshahi, Alireza Aliabadi, Maedeh Mohammadi et al.
Russian Journal of Bioorganic Chemistry
Synthesis and biological activity
article

Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects

Leila Hosseinzadeh, Hossein Malekshahi, Alireza Aliabadi, Maedeh Mohammadi, Amin Hosseini, Ghazal Mahmoudi
article en

Abstract

Objective: Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. Methods: In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. Results and Discussion: Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (VI), (VII), (VIII), (IX), and (XII) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (VII) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (VI–IX), and (XII), just and just, 2-F derivative (IV) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. Conclusions: The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.

Russian Journal of Bioorganic ChemistryVol. 50(6)
Kermanshah University of Medical Sciences (IR)
Openalex Percentile: Top 83%
Synthesis and biological activity
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Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects — Leila Hosseinzadeh, Hossein Malekshahi, et al. · Russian Journal of Bioorganic Chemistry (2024) | TGRS Research Map | TGRS