Abstract

This work includes the synthesis of a series of O- and P- rich platinum complexes by the reaction of Pt+2 with tertiary phosphines (PPh3, dppm, dppe, dppp, dppf) and 3,4,5‑trimethoxybenzoic acid (HTMB) through a one-pot reaction. All complexes were characterized using FTIR, CHN, molar conductivity, 1H NMR and 31P NMR. The characterization results proved that the TMB ligand in all complexes behaves as a monodentate through the deprotonated oxygen atom. The phosphine ligands were associated to platinum center with chelating bidentate mode while PPh3 and dppm were behaved as monodentate and bridging bidentate ligands, respectively. The PPh3-containing complex (trans-[Pt(TMB)2(PPh3)2]) was used to examine its anticancer activity against A2780, SW620, HT29, A172, C6 and HeLa cell lines. The results proved that the TGI value was 40.33 ± 1.4, 18.05 ± 0.8, 48.91 ± 1.6, 44.43 ± 2.8, 51.03 ± 2.0 and 56.98 ± 2.1 for A172, C6, HeLa, A2780, SW620 and HT29, respectively. TGI values were better than those reported for the reference compound 5FU. The molecular docking proves that trans-[Pt(TMB)2(PPh3)2] have pi-alkyl hydrophobic interaction, carbon-hydrogen bonding, electrostatic interaction and pi-lone pair interaction with different amino acids.

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