Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study
Zein, N., Shaban, S., Shafek, S., Baghi, H., Aiad, I., Omran, M. (2021). Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study. EKB Journal Management System, 64(8), 4005-4015. doi: 10.21608/ejchem.2021.64760.3386
Nabila Zein; Samy M. Shaban; Samir Hosny Shafek; Hamza Baghi; I. Aiad; Mervat Omran. "Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study". EKB Journal Management System, 64, 8, 2021, 4005-4015. doi: 10.21608/ejchem.2021.64760.3386
Zein, N., Shaban, S., Shafek, S., Baghi, H., Aiad, I., Omran, M. (2021). 'Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study', EKB Journal Management System, 64(8), pp. 4005-4015. doi: 10.21608/ejchem.2021.64760.3386
Zein, N., Shaban, S., Shafek, S., Baghi, H., Aiad, I., Omran, M. Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study. EKB Journal Management System, 2021; 64(8): 4005-4015. doi: 10.21608/ejchem.2021.64760.3386

Synthesis and characterization of new 1,2,4-triazole anticancer scaffold derivatives: In Vitro study

Egyptian Journal of Chemistry
Article 4, Volume 64, Issue 8, August 2021, Page 4005-4015  XML PDF (759.33 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2021.64760.3386
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Authors
Nabila Zein1; Samy M. Shaban2, 3; Samir Hosny Shafek email 3; Hamza Baghi1; I. Aiad3; Mervat Omran4
1Biochemistry Division, Chemistry Department Faculty of Science, Zagazig University, Egypt
2School of Chemical Engineering, Sungkyunkwan University (SKKU), Suwon 16419, Republic of Korea.
3Egyptian Petroleum Research Institute, Cairo, Egypt.
4Pharmacology Unit, Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, Egypt
Abstract
Four Schiff bases were obtained via one direct click reaction between 3-amino-1H-1,2,4-triazole and different substituted benzaldehyde. The synthesized compounds were characterized on the basis of their spectral data including IR spectra and 1HNMR. The synthesized compounds were tested against three human cancer cell lines to evaluate their in vitro anticancer activity, and also tested on Vero cells extracted from African green monkey kidney to investigate their side effect. The screening showed that the Schiff bases TB-NO2 and TB-OCH3 produced an effective anticancer activity against HEPG2, HCT-116, and MCF-7 cell lines. Further investigations were performed to determine the apoptotic and antifibrotic ability of TB-NO2 and TB-OCH3 on MCF-7 cells by determining the expression of Bax, Bcl-2, CTGF, and PDGF. Results of Bax/Bcl-2 ratio for TB-NO2 and TB-OCH3 confirmed the apoptotic effect of these compounds on MCF-7 cells. The reduction in CTGF and PDGF genes expression confirmed the regulatory effect of these compounds on MCF-7 cells growth.
Keywords
Anticancer activity; 1,2,4-triazole; Schiff base; cytotoxicity; In-vitro
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