Document Type : Original Article
Authors
1
Pharmaceutical organic chemistry , faculty of pharmacy , helwan university, cairo,egypt
2
Pharmaceutical Organic Chemistry Department, Faculty of pharmacy, Helwan University
3
Biochemistry and Molecular Biology Department, Faculty of Pharmacy, Helwan University, , Cairo, Egypt.
4
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain Helwan, Helwan, Egypt.
5
Faculty of pharmacy, Ahram Canadian University, 6th-October, Giza, Egypt
6
Medical Biochemistry Department, National Research Centre, Dokki, Cairo, Egypt
7
1Pharmaceutical Organic Chemistry Department, Faculty of pharmacy, Helwan University
Abstract
Following their synthesis in good to medium yields, pyrrole-pyrimidine-5-cyano scaffolds (2 and 4) were tested for anti-cancer efficacy using the MTT assay against ovarian cancer (SKOV-3) and breast cancer (MCF-7) cell lines. The IC50 values of 1031.135 µg/mL and 846.4994 μg/mL, respectively, were obtained from cytotoxicity assays conducted on the SKOV-3 and MCF-7 cell lines, which demonstrated a substantial decrease in cell viability. Apoptosis and Cell cycle arrest were also carried out to configure the primary contact with cancer cell lines, and N-pyrrole-pyrimidine-5-cyano 2a demonstrated the most anti-cancer efficacy against both tested cell lines in the in vitro assay. Additionally, the molecular docking research revealed that compound (2a) interacts significantly with active sites of Cyclin-dependent kinase 2 (CDK-2) (PDB: 5ANJ) and Cyclin-dependent kinase 6 (CDK-6) (PDB: 5LT2). In order to determine the primary method of action, enzymatic assays were also conducted on CDK2 and CDK6 utilizing specialized Enzyme-Linked Immunosorbent Assay (ELISA) Kits. Our findings indicated that compound (2a) has the potential to be an effective cancer treatment.
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