Synthesis, anti-cancer evaluation and in vitro study of some novel pyrrolo-pyrimidine scaffolds | ||
| Egyptian Journal of Chemistry | ||
| Articles in Press, Accepted Manuscript, Available Online from 27 January 2025 | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2025.340559.10906 | ||
| Authors | ||
| Mariem El Saeed Mohamed* 1; Samar S. Fatahala2; Rania Helmy Abd El-Hameed3; Hanaa B Atya4; Amira Ibrahim Sayed5; Mosaad Sayed Mohamed6; Omnia Aly7 | ||
| 1Pharmaceutical organic chemistry , faculty of pharmacy , helwan university, cairo,egypt | ||
| 2Pharmaceutical Organic Chemistry Department, Faculty of pharmacy, Helwan University | ||
| 3Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain Helwan, Helwan, Egypt. | ||
| 4Biochemistry and Molecular Biology Department, Faculty of Pharmacy, Helwan University, , Cairo, Egypt. | ||
| 5Faculty of pharmacy, Ahram Canadian University, 6th-October, Giza, Egypt | ||
| 61Pharmaceutical Organic Chemistry Department, Faculty of pharmacy, Helwan University | ||
| 7Medical Biochemistry Department, National Research Centre, Dokki, Cairo, Egypt | ||
| 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. | ||
| Keywords | ||
| CDK-2; CDK-6; anti-cancer; pyrimidine; pyrrole | ||
|
Statistics Article View: 161 |
||
