Heterocycles are key structural components of many of the anti-cancer drugs available on the market today. Indeed, of the novel molecular anti-cancer agents approved by the FDA between 2010 and 2015, almost two-thirds contained heterocyclic rings within their structures.
Their prevalence in anti-cancer drug design can be partly attributed to their being extremely common in nature, with a vast number of cellular processes and mechanisms having evolved the ability to interact with them. Their versatility means there are multiple metabolic pathways and cellular processes within cancer pathology that can be susceptible to heterocycle-based drugs.
In this article, we look at some of the most important heterocyclic compounds currently implicated in cancer therapy, both on the market and in development, discuss the properties that make them valuable as anti-cancer drugs, and consider the benefits of including heterocycles within high-throughput screening libraries.
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