The indole subunit is a near-ubiquitous component of biologically active natural products, and its study has been a major focus of research for generations. Substituted indoles have frequently been referred to as privileged structures since they are capable of binding to multiple receptors with high affinity, and thus have applications across a wide range of therapeutic areas. Due to this activity, it is not surprising that the indole ring system has become an important building block or intermediate in the synthesis of many pharmaceutical agents. Notably, indole-3-carbinol, found in cruciferous vegetables, inhibits carcinogenesis at the initiation stage and has been shown to inhibit carcinogenesis in several animal species; but, it enhances tumor incidence if administered at a post-initiation stage.

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Indoles and Indole Isosteres