Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view

Eur J Med Chem. 2017 Jul 7:134:159-184. doi: 10.1016/j.ejmech.2017.04.003. Epub 2017 Apr 5.

Abstract

Indoles constitute extensively explored heterocyclic ring systems with wide range of applications in pathophysiological conditions that is, cancer, microbial and viral infections, inflammation, depression, migraine, emesis, hypertension, etc. Presence of indole nucleus in amino acid tryptophan makes it prominent in phytoconstituents such as perfumes, neurotransmitters, auxins (plant hormones), indole alkaloids etc. The interesting molecular architecture of indole makes them suitable candidates for the drug development. This review article provides an overview of the chemistry, biology, and toxicology of indoles focusing on their application as drugs. Our effort is to corroborate the information available on the natural indole alkaloids, indole based FDA approved drugs and clinical trial candidates having diverse therapeutic implementations. This compiled information may serve as a benchmark for the alteration of existing ligands to design novel potent molecules with lesser side effects.

Keywords: Antiemetic; Antimicrobial; Antiviral; Cancer; Indole; Migraine.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Anti-Infective Agents / therapeutic use
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Antiemetics / chemistry
  • Antiemetics / pharmacology
  • Antiemetics / therapeutic use
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Bacterial Infections / drug therapy
  • Chemistry, Pharmaceutical
  • Cholinergic Antagonists / chemistry
  • Cholinergic Antagonists / pharmacology
  • Cholinergic Antagonists / therapeutic use
  • Drug Discovery* / methods
  • Humans
  • Indoles / chemistry*
  • Indoles / pharmacology*
  • Indoles / therapeutic use
  • Migraine Disorders / drug therapy
  • Mycoses / drug therapy
  • Neoplasms / drug therapy
  • Virus Diseases / drug therapy

Substances

  • Anti-Infective Agents
  • Anti-Inflammatory Agents
  • Antiemetics
  • Antineoplastic Agents
  • Cholinergic Antagonists
  • Indoles