Nowadaysthere has been a significant increase in interest in 5-HT7 and 5-HT5A receptors in the context of cancer treatment.The possible role of 5-HT6R in the pathogenesis and progressionof glioma remains an interesting and relatively unexplored issue.We developed a new group of long-chain 2-aminoquinazoline sulfonamidesas new multifunctional serotonin receptor ligands, focused on 5-HT6R. The chosen group was further evaluated for antiproliferativeeffects on 1321N1 astrocytoma cells, along with U87MG, U-251, andLN-229 glioblastoma cell lines. The gene discussed is HTR6; the disease is central nervous system cancer.