Efficient procedure for preparation of the novel magnetic nanobiocomposite (MNbC) was successfully established by employing click chemistry protocol. The resulted structure exhibited valuable characteristics from biological viewpoints. The prepared materials and obtained nanobiocomposite were characterized by means of nuclear magnetic resonance (NMR), fourier transform infrared (FT-IR), thermal gravimetric analysis (TGA) and differential scanning calorimetry (DSC). To assay the antiproliferative effects of the MNbC; as cancerous cells, Hela, MCF-7 and Saos were evaluated by means of MTT assay and compared with normal fibroblast cell line. Promising antiproliferative effects were observed on both epitheloid and mesenchymal cancer cell lines depending on MNbC concentration and time. To detect the apoptosis-associated changes of cell membranes during the process of apoptosis, Acridine Orange/Ethidium Bromide (AO/EB) dual staining fluorescent technique was incorporated. The studies in this article including all of these specifications represent convincing key findings that make MNbC as an appreciable candidate for further bio-applications.