科研之友
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摘要
The availability of chemical and biological data presented in this paper is the basis for understanding not only the current state of anti-cancer drugs based on gold(Ⅲ), but also the rationale for strategies for future drug design. New Au(Ⅲ) nanosized complexes of cefotaxime(ceph-3) and cefepime(ceph-4) ligands as a 3 rd and 4 th of cephalosporin generation drugs were synthesized. Gold(Ⅲ) complexes were discussed based on the elemental, molar conductance, thermal and magnetic moment measurements as well as spectral(FTIR, 1HNMR, UV-Vis, and XRD) techniques. FT-IR spectra revealed that the ceph-3 and ceph-4 ligands reacted as a bidentate ligands through carboxylate oxygen and β-lactam oxygen groups. The analytical analysis confirm that the molar ratio is 1∶1(Au3+/ceph) with general formula [Au(L)(Cl)2] where L=ceph-3 or ceph-4. The structures of Au(Ⅲ) complexes were presence as a square planar geometry. X-ray diffraction patterns referred to a crystalline nature for all synthesized complexes. TEM analyses confirmed that the synthetic gold(Ⅲ) complexes have a nanosized particles. In vitro antimicrobial activities of Au(Ⅲ) complexes were evaluated towards two types of bacteria(G+ & G-). The antitumor activities of gold(Ⅲ) complexes are appraised against breast(MCF-7) and colorectal adenocarcinoma(Caco-2) cell lines, which means that the two complexes may consider promising anticancer drugs.
