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Tavallaei, Omid, Heidarian, Milad, Marzbany, Marzieh, Aliabadi, Alireza. (1400). Cytotoxicity and pro‐apoptosis activity of synthetic 1,3-thiazole incorporated phthalimide derivatives on cancer cells. , 24(5), 604-614. doi: 10.22038/ijbms.2021.53845.12103
Omid Tavallaei; Milad Heidarian; Marzieh Marzbany; Alireza Aliabadi. "Cytotoxicity and pro‐apoptosis activity of synthetic 1,3-thiazole incorporated phthalimide derivatives on cancer cells". , 24, 5, 1400, 604-614. doi: 10.22038/ijbms.2021.53845.12103
Tavallaei, Omid, Heidarian, Milad, Marzbany, Marzieh, Aliabadi, Alireza. (1400). 'Cytotoxicity and pro‐apoptosis activity of synthetic 1,3-thiazole incorporated phthalimide derivatives on cancer cells', , 24(5), pp. 604-614. doi: 10.22038/ijbms.2021.53845.12103
Tavallaei, Omid, Heidarian, Milad, Marzbany, Marzieh, Aliabadi, Alireza. Cytotoxicity and pro‐apoptosis activity of synthetic 1,3-thiazole incorporated phthalimide derivatives on cancer cells. , 1400; 24(5): 604-614. doi: 10.22038/ijbms.2021.53845.12103

Cytotoxicity and pro‐apoptosis activity of synthetic 1,3-thiazole incorporated phthalimide derivatives on cancer cells

Iranian Journal of Basic Medical Sciences
مقاله 6، دوره 24، شماره 5، مرداد 2021، صفحه 604-614    اصل مقاله (673.17 K)
نوع مقاله: Original Article
شناسه دیجیتال (DOI): 10.22038/ijbms.2021.53845.12103
نویسندگان
Omid Tavallaei1، 2؛ Milad Heidarian2، 3؛ Marzieh Marzbany1، 2؛ Alireza Aliabadi* 1، 4
1Pharmaceutical Sciences Research Center, Health Institute, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
2Department of Pharmacognosy and Pharmaceutical Biotechnology, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
3Students Research Committee, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
4Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
چکیده
Objective(s): Cancer is the second important reason for death worldwide. In spite of advances in cancer treatment, however, survival of patients stays weak. Therefore, there is a critical need for advancement of new anticancer drugs. Regarding the hopeful biological activity of phthalimide derivatives, in this study, synthesis, cytotoxicity, and pro‐apoptosis activity of eleven derivatives of thiazole bearing phthalimide structure were evaluated.
Materials and Methods: First, target derivatives were synthesized. All synthesized compounds were characterized by spectroscopic methods. Cytotoxicity and pro‐apoptosis activity of the synthesized compounds were evaluated in MDA-MB-468, PC-12, and MCF-7 cancer cell lines by MTT assay, caspase-3 activity, and TUNEL assay. Finally, expression of BAX, BCL-2, and FAS (as markers of apoptosis) was assessed by the RT-PCR procedure.
Results: Among the eleven compounds, 5b (IC50 = 0.2±0.01 µM) was found to be the most potent derivative against MCF-7 cells. Also, Compound 5k and 5g showed strong cytotoxic activity against MDA-MB-468 and PC-12 cells with IC50 value of 0.6±0.04 µM and 0.43±0.06 µM, respectively.  DNA fragmentation and activity of caspase-3 data suggest that cytotoxic activity of the compounds on cancer cells might be related to apoptosis. Also, RT-PCR of apoptosis markers indicated that these compounds induce apoptosis through the intrinsic pathway.
Conclusion: Our findings suggest that para chloro derivative (5c) may be a promising agent for treatment of cancer cells by the targeted intrinsic pathway of apoptosis and could be used as a drug candidate for in vivo assessment in the treatment of cancer.
کلیدواژه‌ها
Apoptosis؛ Cancer cells؛ Cytotoxicity؛ Phthalimide؛ Thiazole
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