Recent research tried to analyze the conjugation of some chemotherapeutic drugs to the biologically produced gold nanoparticles (GNPs) in one step, without the use of any additional linkers. GNPs was produced using Fusarium oxysporum and their presence was confirmed using spectrophotometer, transmission electron microscope (TEM), X-ray diffraction (XRD) and fourier transform infrared (FTIR) analyses. In order to carry out the conjugation study, capecitabine, tamoxifen, and paclitaxel were added dropwise to the GNPs solution under stirring condition and spectrophotometer, dynamic light scattering (DLS) and FTIR analyses were performed to prove the successful conjugation. Finally, AGS and MCF7 cell lines were used for methyl thiazol tetrazolium (MTT) assay to determine the toxicity of each drug and its conjugated form. Results showed that the spherical and hexagonal GNPs with maximum absorbance peak around 524 nm and average sizes less than 20 nm were produced. FTIR analysis clarified the presence of proteins on the surfaces of the GNPs. After the conjugation process although the FTIR analysis demonstrated that all the drugs were successfully conjugated to GNPs, MTT assay revealed that unlike the paclitaxel conjugated GNPs, capecitabine and tamoxifen conjugates displayed no toxic effects due to their deactivation and low half-lives. Moreover the average size and polydispersity index (PDI) of the GNPs after conjugation with all the three tested drugs increased. In conclusion different types of drugs could conjugate to the GNPs but it is important to employ high stable forms of the drugs in the conjugation procedure.