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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 3rd and 4th 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 , 1 HNMR ,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 andβ-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 patts re-ferred 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 evalua-ted 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 comple-xes may consider promising anticancer drugs .