Design and Synthesis of Novel Pyrazoles, Pyrazolines, and Pyridines from Chalcone Derivatives with Evaluation of Their In Vitro Anticancer Activity Against T-47D and UACC-257 Cell Lines
Mangoud, M., Hussein, M., El-Bordany, E. (2020). Design and Synthesis of Novel Pyrazoles, Pyrazolines, and Pyridines from Chalcone Derivatives with Evaluation of Their In Vitro Anticancer Activity Against T-47D and UACC-257 Cell Lines. EKB Journal Management System, 63(12), 5203-5218. doi: 10.21608/ejchem.2020.28793.2620
Mangoud Mohamed Mangoud; Mohamed Zaki Hussein; Eman A. El-Bordany. "Design and Synthesis of Novel Pyrazoles, Pyrazolines, and Pyridines from Chalcone Derivatives with Evaluation of Their In Vitro Anticancer Activity Against T-47D and UACC-257 Cell Lines". EKB Journal Management System, 63, 12, 2020, 5203-5218. doi: 10.21608/ejchem.2020.28793.2620
Mangoud, M., Hussein, M., El-Bordany, E. (2020). 'Design and Synthesis of Novel Pyrazoles, Pyrazolines, and Pyridines from Chalcone Derivatives with Evaluation of Their In Vitro Anticancer Activity Against T-47D and UACC-257 Cell Lines', EKB Journal Management System, 63(12), pp. 5203-5218. doi: 10.21608/ejchem.2020.28793.2620
Mangoud, M., Hussein, M., El-Bordany, E. Design and Synthesis of Novel Pyrazoles, Pyrazolines, and Pyridines from Chalcone Derivatives with Evaluation of Their In Vitro Anticancer Activity Against T-47D and UACC-257 Cell Lines. EKB Journal Management System, 2020; 63(12): 5203-5218. doi: 10.21608/ejchem.2020.28793.2620

Design and Synthesis of Novel Pyrazoles, Pyrazolines, and Pyridines from Chalcone Derivatives with Evaluation of Their In Vitro Anticancer Activity Against T-47D and UACC-257 Cell Lines

Egyptian Journal of Chemistry
Article 45, Volume 63, Issue 12, December 2020, Page 5203-5218  XML PDF (2.1 MB)
Document Type: Original Article
DOI: 10.21608/ejchem.2020.28793.2620
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Authors
Mangoud Mohamed Mangoud email orcid 1; Mohamed Zaki Hussein2; Eman A. El-Bordanyorcid 3
14 Ibn Khaldoun Square
2Environmental Research Department, National Center for Social and Criminological Research, Ibn Khaldoun Square, Mohandesin, Zamalek, Giza 11561, Egypt
3Department of Chemistry, Faculty of Science, Ain Shams University, Cairo 32511, Egypt
Abstract
Novel series of pyrazoline carbothioamides, acetyl pyrazoles, pyridine-3-carbonitriles, pyridine-2-carbonitriles, and nicotinonitriles were synthesized. The structures of the newly synthesized compounds were established based on their spectral data, elemental analyses and alternative synthetic routes whenever possible. Also, the newly synthesized compounds were screened for their in vitro anticancer activity against T-47D (breast cancer human cell line) and UACC-257 (melanoma human cell line) by MTT assay (a colorimetric assay for assessing cell metabolic activity). Experimental results demonstrated that compounds 3a, 4a, and 8c showed excellent in vitro activity against T-47D cell line, while compounds 3d, 6d, and 5b exhibited excellent activity against UACC-257 cell line. Molecular docking studies were performed on compound 4a, as it showed the most promising activity against T-47D cell line, using Molecular Operation Environment (MOE 2008.10) software. Also, drug-likeness, pharmacokinetics, and toxicity assessment studies were carried out.
Keywords
Anticancer; docking; pharmacokinetics; chalcones; pyrazolines; carbonitriles; cyanopyridines
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