Oxindole: A chemical prism carrying plethora of therapeutic benefits

Eur J Med Chem. 2016 Nov 10:123:858-894. doi: 10.1016/j.ejmech.2016.08.011. Epub 2016 Aug 8.

Abstract

Oxindole has emerged as a valuable scaffold in medicinal chemistry possessing diverse range of pharmacological activities. Its value has further been increased by its natural occurrence as alkaloids in variety of plants. It was first extracted from the cat claw's plant Uncaria tomentosa found in the Amazon rainforest and other tropical areas of South and Central America. Traditionally as well as present emerging therapeutic potential of oxindole nucleus has captured the interest of medicinal chemists to synthesize novel oxindole derivatives. In the present review the authors have integrated its chemistry and synthetic strategies developed after 1945. Also the information of naturally occurring oxindole alkaloids has been incorporated. The detailed pharmacological activities including anti-cancer, anti-HIV, antidiabetic, antibacterial, antioxidant, kinase inhibitory, AChE inhibitory, anti-leishmanial, β3 adrenergic receptor agonistic, phosphatase inhibitory, analgesic, spermicidal, vasopressin antagonists, progesterone antagonists, neuroprotection, and NMDA blocker activities of oxindole derivatives alongwith their SAR has also been discussed in detail. Additionally, information regarding the oxindole derivatives in clinical trials has been incorporated. Thus, this review will provide insights for the synthetic as well as medicinal chemist for the designing and synthesis of novel oxindole derivatives with novel improved range of pharmacological implications.

Keywords: Anti-cancer; Anti-oxidant; Kinase inhibitory activity; Oxindole; Sunitinib.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Humans
  • Indoles / chemistry*
  • Indoles / pharmacology*
  • Indoles / therapeutic use
  • Oxindoles

Substances

  • Indoles
  • Oxindoles
  • 2-oxindole