Synthesis, Characterization and Biological Activity of Some New Phthalazine Derivatives | ||
| Advances in Environmental and Life Sciences | ||
| Articles in Press, Accepted Manuscript, Available Online from 11 September 2025 | ||
| Document Type: Original research articles | ||
| DOI: 10.21608/aels.2025.376483.1075 | ||
| Authors | ||
| Samir Elrayes* 1; Ibrahim Ahmed Ibrahim2; ahmed hussein3 | ||
| 1Chemistry department, Faculty of Sciences, Suez Canal University | ||
| 2Department of chemistry, faculty of science, Suez canal university, Ismailia | ||
| 3chemistry department Suez canal university | ||
| Abstract | ||
| A number of new substituted phthalazine derivatives have been created and manufactured to block the vascular endothelial growth factor receptor (VEGFR) kinase enzyme in an attempt to create novel targeted anticancer medicines. Structure-activity relationship (SAR) analyses of well-known VEGFR inhibitors served as the basis for this. The compounds have an N-substituted piperazine located at site 1 of the phthalazine nucleus, or they have a bis acrylamide or biarylurea dick connected to a phthalazine structure through an amino or either connection. The produced compounds' ability to inhibit VEGFR-2 kinase was assessed. Interestingly, three of the phthalazines with a biarylurea showed good broad-spectrum suppression of cell growth anti the NCI 60 cell panel, with IC50 power between 0.16 and 5 μM. If we want to learn more about these drugs' binding connection and correspondence with the VEGFR-2 kinase, docking experiments were also carried out by simulating their interlinkage with the VEGFR-2 binding site. The synthesis of structures incorporating the phthalazine moiety has been the focus of numerous experimental experiments. Creating an effective process for creating heterocyclic compounds with this moiety is still a major difficulty. We used regression analysis and the quantitative structure-activity relationship (QSAR) in our continuous search for novel candidates that could be useful in creating strong, specific, and less harmful anticancer drugs. This technique tries to anticipate novel heterocycles containing the phthalazine component, which could work for as dummy for the creation of novel anticancer drugs. | ||
| Keywords | ||
| Anticancer; Phthalazines; Cytotoxic; Peptide | ||
|
Statistics Article View: 4 |
||
