Recent Updates on Indole Derivatives as Kinase Inhibitors in the Treatment of Cancer

Anticancer Agents Med Chem. 2023;23(4):404-416. doi: 10.2174/1871520622666220607143040.

Abstract

Cancer is becoming a global threat as its treatment accounts for many challenges. Hence, newer inventions prioritize the requirement of developing novel anticancer agents. In this context, kinases have been exclusively investigated and developed as a promising and novel class of drug targets for anticancer regimen. Indole derivatives have been found to be most effective for targeting multiple kinases, such as PIM, CDK, TK, AKT, SRC, PI3K, PKD, GSK, etc., to inhibit cell proliferation for cancer. Recently, a group of researchers have proposed their research outcomes related to this moiety, such as Zhang et al. described some potent PI3K inhibitors by substitution at the 4th position of the indole ring. Kassis et al. enumerated several potent CDK5 inhibitors by substituting the 2nd and 6th positions of the indole ring. In the present review, we have taken the initiative to summarize structure-activity relationship (SAR) studies of indole derivatives as kinase inhibitors for the development of potential inhibitors.

Keywords: CDK5 inhibition; Indole derivatives; SAR; cancer; clinical trial; kinases.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Cell Proliferation
  • Humans
  • Indoles / pharmacology
  • Indoles / therapeutic use
  • Molecular Structure
  • Neoplasms* / drug therapy
  • Phosphatidylinositol 3-Kinases
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Structure-Activity Relationship

Substances

  • Phosphatidylinositol 3-Kinases
  • Antineoplastic Agents
  • Indoles
  • Protein Kinase Inhibitors