Abstract
Four pyrazolone derivatives and their corresponding silver complexes were synthesized and characterized. Based on elemental analysis, 1 : 2 (M : L) molar ratio was suggested for all inspected complexes. 1H, 13C NMR, mass, UV-Vis, TGA, and IR were the spectral tools used for describing the formulae. Moreover, XRD patterns and SEM pictures were used to evaluate the particle sizes which appeared strongly in nanometer range. CT-DNA study is the major consideration in this study, to test the interacting ability of all synthesized cationic complexes towards cell DNA. Each binding constant was computed and correlated with the Hammett sigma constant. Antitumor activity was examined upon three carcinoma cell lines (MCF-7, HepG2, and HCT116). The high efficiency was recorded towards MCF-7 (breast carcinoma) cell line. Kinetic studies yield essential parameters to assert on the rule of metal atom on thermal feature of organic compounds. Molecular modeling was implemented to optimize the structures of compounds. Also, molecular docking was achieved to obtain a clear view about proposed drug behavior within the affected cells. This was achieved through comparing the calculated internal energy values of all docking complexes. All the tested compounds displayed a significant interaction with breast cancer protein (strong matching with practical result) followed by DNA polymerase protein.
Highlights
After discovering the cisplatin as an effective antitumor drug, the interest of researchers in the coordination chemistry increased to design highly effective complexes as antiantitumor operators [1,2,3]
The limitations of the clinical success of cisplatin due to critical side effects and resistance that cause retrogression [4] have stimulated searches for other metal complexes. e synthesis for series silver(I) complexes as antitumor agents conquers a considerable place in cancer chemotherapy, as evidenced by their remarkable therapeutic potential reflected in many reported research works [5]. e silver ion is of considerable solicitude in the design of coordination complexes due to the resilience of its coordination sphere and the ease with which it varies its coordination number
Based on all of the afore-mention, we focused in this work on the synthesis of nonpolymeric silver complexes with pyrazolone to improve its e ciency as anticancer drug for three carcinoma cell lines and to study their interaction with DNA. e structure of novel complexes will be investigated through all possible spectral and analytical tools
Summary
After discovering the cisplatin as an effective antitumor drug, the interest of researchers in the coordination chemistry increased to design highly effective complexes as antiantitumor operators [1,2,3]. E synthesis for series silver(I) complexes as antitumor agents conquers a considerable place in cancer chemotherapy, as evidenced by their remarkable therapeutic potential reflected in many reported research works [5]. E silver ion is of considerable solicitude in the design of coordination complexes due to the resilience of its coordination sphere and the ease with which it varies its coordination number (from 2 to 4, rarely 5 or 6). Coordination complexes of silver are known to be convertible through changes in ligand geometry, rigidity or functionality, and/or by modifications to the counter-ion or solvent system [6]. The wide range of biological activities of pyrazolone as antitumor [12], anti-inflammatory [13] and antimicrobial
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