Styrylquinolines Derivatives: SAR Study and Synthetic Approaches

Med Chem. 2022;18(8):859-870. doi: 10.2174/1573406418666220214085856.

Abstract

In the present-day scenario, heterocyclic derivatives have revealed the primary function of various medicinal agents precious for humanity. Out of a diverse range of heterocycles, Styrylquinolines scaffolds have been proved to play an essential role in a broad range of biological activities, including anti-HIV-1, antimicrobial, anti-inflammatory, anti-Alzheimer activity with antiproliferative effects on tumor cell lines. Due to the immense pharmacological importance, distinct synthetic methods have been executed to attain new drug entities from Styrylquinolines. Various schemes for synthesizing Styrylquinolines derivatives like one-pot, ultrasound-promoted heterogeneous acid-catalysed, microwave-assisted, solvent-free, and green synthesis were discussed in the present review. Some products of Styrylquinolines are in clinical trials, and patents are also granted for the novel synthesis of Styrylquinolines. According to the structure-activity relationship, replacement at the R-7 and R-8 positions is required for various activities. In this review, recent synthetic approaches in the medicinal chemistry of Styrylquinolines and potent Styrylquinolines derivatives based on structural activity relationships (SAR) are outlined. Moreover, their primary methods and modifications are also discussed.

Keywords: Heterocycles; SAR study; quinoline; styryl moiety; styrylquinolines; synthetic schemes.

Publication types

  • Review

MeSH terms

  • Anti-Inflammatory Agents / pharmacology
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical
  • Quinolines* / chemistry
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Quinolines
  • styrylquinoline