Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets

Pharmacol Ther. 2024 Feb:254:108579. doi: 10.1016/j.pharmthera.2023.108579. Epub 2023 Dec 30.

Abstract

Cancer, a noncommunicable disease, is the leading cause of mortality worldwide and is anticipated to rise by 75% in the next two decades, reaching approximately 25 million cases. Traditional cancer treatments, such as radiotherapy and surgery, have shown limited success in reducing cancer incidence. As a result, the focus of cancer chemotherapy has switched to the development of novel small molecule antitumor agents as an alternate strategy for combating and managing cancer rates. Heterocyclic compounds are such agents that bind to specific residues in target proteins, inhibiting their function and potentially providing cancer treatment. This review focuses on privileged heterocyclic pharmacophores with potent activity against carbonic anhydrases and kinases, which are important anticancer targets. Evaluation of ongoing pre-clinical and clinical research of heterocyclic compounds with potential therapeutic value against a variety of malignancies as well as the provision of a concise summary of the role of heterocyclic scaffolds in various chemotherapy protocols have also been discussed. The main objective of the article is to highlight key heterocyclic scaffolds involved in recent anticancer drug design that demands further attention from the drug development community to find more effective and safer targeted small-molecule anticancer agents.

Keywords: Cancer treatment; Carbonic anhydrases; Drug design; Heterocyclic; Kinases; Pharmacology; Targeted anticancer drugs.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Drug Design
  • Drug Development
  • Heterocyclic Compounds* / pharmacology
  • Heterocyclic Compounds* / therapeutic use
  • Humans
  • Neoplasms* / drug therapy

Substances

  • Antineoplastic Agents
  • Heterocyclic Compounds