Synthesis, biological assessment, and docking study of new pyrazolo[1,5-a]pyrimidine derivatives with potential anticancer activity. | ||
| Azhar International Journal of Pharmaceutical and Medical Sciences | ||
| Article 24, Volume 5, Issue 1, January 2025, Pages 288-296 PDF (680.37 K) | ||
| Document Type: Original research articles | ||
| DOI: 10.21608/aijpms.2024.294539.1271 | ||
| Authors | ||
| Yasmin AE Shafei* 1; Rehab Sabour2; Nadia M Mahfouz3, 4; Heba SA Elzahabi2 | ||
| 1Department of Chemistry, Faculty of Pharmacy, October 6 University, Giza, Egypt | ||
| 2Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt | ||
| 3Department of Chemistry, Faculty of Pharmacy, October 6 University, Gize, Egypt | ||
| 4Medicinal Chemistry, Faculty of Pharmacy, Assuit University, Assuit, Egypt | ||
| Abstract | ||
| Cancer is described as malignant cell proliferation. Normal cells lose control of their regulatory activities, which result in abnormal growth and division. Novel series of pyrazolo[1,5-a]pyrimidine analogues have been synthesized and assessed for anti-proliferative effect based on different studies focused on the significance of the pyrazolo[1,5-a]pyrimidine framework in tumor progression management. To assess the novel hits' antitumor efficacy, three tumor cell lines have been employed: MCF-7 for breast, HepG2 for liver, in addition to A549 for lung. According to cytotoxic screening, Compound 4d has been found to exhibit greater activity over doxorubicin, as shown by its IC50 = 0.72 ± 0.03 μM for MCF- 7 and IC50 = 0.14 ± 0.54 μM for HepG2 cell lines. Furthermore, it demonstrated a significant effect on the A549 cell line, exhibiting an IC50 = 2.33 ± 0.61 μM in comparison to doxorubicin (IC50 = 2.28, 3.67 and 2.62 μM respectively). Moreover, molecular docking of 4d has been achieved to highlight its binding interactions and affinity for the VEGFR-2 enzyme active site. Also, in silico results indicated that all compounds (4a-e) have high absorption while they can't cross the blood brain barrier. | ||
| Keywords | ||
| pyrazolo[1,5-a]pyrimidine; Synthesis; Anticancer; Docking modelling | ||
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