Synthesis, Characterization, Cytotoxicity Study and Docking Studies of New Fused-pyrazoline Derivatives derived from Bis-Chalcones Against Breast Cancer cells
Alidmat, M., Ning, T., Khairuddean, M., Shayazi, N., Nik Mohammad Kamal, N., Muhammad, M. (2021). Synthesis, Characterization, Cytotoxicity Study and Docking Studies of New Fused-pyrazoline Derivatives derived from Bis-Chalcones Against Breast Cancer cells. EKB Journal Management System, 64(12), 6901-6911. doi: 10.21608/ejchem.2021.73796.3648
Mohammad Murwih Alidmat; Tan Zhi Ning; Melati Khairuddean; Nurul Hayati Shayazi; Nik Nur Syazni Nik Mohammad Kamal; Musthahimah Muhammad. "Synthesis, Characterization, Cytotoxicity Study and Docking Studies of New Fused-pyrazoline Derivatives derived from Bis-Chalcones Against Breast Cancer cells". EKB Journal Management System, 64, 12, 2021, 6901-6911. doi: 10.21608/ejchem.2021.73796.3648
Alidmat, M., Ning, T., Khairuddean, M., Shayazi, N., Nik Mohammad Kamal, N., Muhammad, M. (2021). 'Synthesis, Characterization, Cytotoxicity Study and Docking Studies of New Fused-pyrazoline Derivatives derived from Bis-Chalcones Against Breast Cancer cells', EKB Journal Management System, 64(12), pp. 6901-6911. doi: 10.21608/ejchem.2021.73796.3648
Alidmat, M., Ning, T., Khairuddean, M., Shayazi, N., Nik Mohammad Kamal, N., Muhammad, M. Synthesis, Characterization, Cytotoxicity Study and Docking Studies of New Fused-pyrazoline Derivatives derived from Bis-Chalcones Against Breast Cancer cells. EKB Journal Management System, 2021; 64(12): 6901-6911. doi: 10.21608/ejchem.2021.73796.3648

Synthesis, Characterization, Cytotoxicity Study and Docking Studies of New Fused-pyrazoline Derivatives derived from Bis-Chalcones Against Breast Cancer cells

Egyptian Journal of Chemistry
Article 2, Volume 64, Issue 12, December 2021, Page 6901-6911  XML PDF (907.02 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2021.73796.3648
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Authors
Mohammad Murwih Alidmat1; Tan Zhi Ning2; Melati Khairuddean email 2; Nurul Hayati Shayazi2; Nik Nur Syazni Nik Mohammad Kamal3; Musthahimah Muhammad3
1School of chemical science Universiti Sains Malaysia
2School of Chemical Sciences, University Sains Malaysia, 11800 Penang, Malaysia
3Advanced Medical and Dental Institute, Universiti Sains Malaysia, 13200 Kepala Batas, Penang, Malaysia
Abstract
Breast cancer is one of the prevalent diseases that kill millions of women worldwide. The development of resistance and side effects of chemotherapy drugs is a common obstacle in the treatment of breast cancer. Recently, the focus of drug discovery has increased toward a valuable structure known as chalcones due to their extensive bioactivity in cancer treatment. In this study, 6 chalcones and 4 fused-pyrazoline derivatives have been synthesized (1-6) using the Claisen-Schmidt condensation technique for cyclopentanone and cyclohexanone with different aromatic aldehydes at room temperature. Chalcones 2-3 and 5-6 were used in cyclo-condensation reaction with thiosemicarbazide to form new fused pyrazoline derivatives. All the synthesized chalcones and fused pyrazoline were characterized using ATR-FTIR, H-NMR and 13C-NMR (1D ). The cytotoxic activity of these new chalcone compounds was investigated against breast cancer cell lines (MCF-7) and normal breast cell lines (MCF-10A). The results showed that compounds 1 and 10 exhibited significant antiproliferative effects against MCF-7 with IC50 values of 8 µM and 8.5 µM when exposed for 48 hours compared with the reference anticancer drug, tamoxifen. Molecular docking analysis showed that compounds 1 and 10 entered the pocket of ERα and interaction with the amino acids in high affinity of binding as tamoxifen.
Keywords
fused-pyrazoline; cyclopentanone; cyclohexanone; Docking Studies; cytotoxicity
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