The synthesis review of the approved tyrosine kinase inhibitors for anticancer therapy in 2015-2020

Bioorg Chem. 2021 Aug:113:105011. doi: 10.1016/j.bioorg.2021.105011. Epub 2021 May 24.

Abstract

In the 21st century, cancer is the major public health problem worldwide. Based on the important roles of protein tyrosine kinase, the accelerated hunt for potent small-molecule tyrosine kinase inhibitors has led to the success of 30 newly inhibitors in this family for the cancer therapy in last five years. In this review, we updated their synthesis methods, and compared the original research routes with the optimized routes for each PTK inhibitor against different target, in order to make an outlook on the future synthesis of potential PTK inhibitors for anticancer therapy.

Keywords: Anticancer drugs; Synthesis routes; Tyrosine kinase inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Agammaglobulinaemia Tyrosine Kinase / antagonists & inhibitors
  • Agammaglobulinaemia Tyrosine Kinase / metabolism
  • Anaplastic Lymphoma Kinase / antagonists & inhibitors
  • Anaplastic Lymphoma Kinase / metabolism
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use*
  • ErbB Receptors / antagonists & inhibitors
  • ErbB Receptors / metabolism
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / metabolism
  • Protein Kinase Inhibitors / therapeutic use
  • Receptors, Platelet-Derived Growth Factor / antagonists & inhibitors
  • Receptors, Platelet-Derived Growth Factor / metabolism
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vascular Endothelial Growth Factor A / metabolism
  • fms-Like Tyrosine Kinase 3 / antagonists & inhibitors
  • fms-Like Tyrosine Kinase 3 / metabolism

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Vascular Endothelial Growth Factor A
  • Anaplastic Lymphoma Kinase
  • ErbB Receptors
  • FLT3 protein, human
  • Receptors, Platelet-Derived Growth Factor
  • fms-Like Tyrosine Kinase 3
  • Agammaglobulinaemia Tyrosine Kinase