DNA is a genetic material with a specialised double-helical structure that is found in both eukaryotic and somatic cells. G-quadruplex is a nucleic acid secondary structure found in guanine-rich sequences of the genome. The G-4 system has been shown to regulate replication, DNA damage repair, and transcription and translation of oncogenes and other cancer-related genes. As a result, targeting G-4 has emerged as a novel and promising anticancer strategy. Small molecules that directly bind to the G-quadruplex and molecules that interfere with the binding between the G-quadruplex structures and related binding proteins have all been designed, synthesised, and identified as potential anti-tumor agents. This review will look at the feasibility of G-quadruplex ligands acting as anti-tumor drugs, from the ground up. In the meantime, since Meanwhile, because helicase is the most well-defined Gquadruplex-related protein, the most extensive research on the relationship between helicase and G-quadruplexes, as well as its implications for drug design, is highlighted.