Cancer remains a critical study since long period. Inspite of remarkable development in science, still suitable cure and treatment is not available. In humans, Hypoxia-inducible factor-1 (HIF-1) is available in good amount in tumors and is associated in various mechanisms such as metabolism of anaerobic energy, angiogenesis, drug resistance, cell subsistence and incursion etc. Hence, for the treatment of cancer, HIF-1 inhibition may be considered as an obvious strategy. Recent studies illustrate many advances in cancer biology and biotechnology for targeting new HIF-1 agents. Numerous heterocyclic compounds are available as anticancer agents and countless struggles have been placed to discover unique agents in the coming years, which can be considered as an important tool for the diagnosis of cancer. This review provides a vision for novel anticancer targets and highlights rationally designed drugs in clinical advancement, and also the budding molecules that can influence clinical care in the coming future. Although several anticancer treatments have been familiarized in the recent years, however, none of them stand up for a better cure and because of which a new and advanced treatment becomes obligatory.