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Updated: May 6, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
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Published on: January 22, 2019

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Structure-Activity Relationship Study and Design Strategies of Hydantoin, Thiazolidinedione, and Rhodanine-Based

Muhammad Naufal1, Elvira Hermawati2, Yana Maolana Syah2

  • 1Department of Chemistry, Padjadjaran University, Jalan Raya Bandung-Sumedang Km. 21, Jatinangor, Sumedang 45363, Indonesia.

ACS Omega
|February 5, 2024
PubMed

Insights

This review details the discovery of Small Molecule Kinase Inhibitors (SMKIs) from 1999-2023. It focuses on developing novel hydantoin, thiazolidinedione, and rhodanine derivatives for targeted cancer therapy.

Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Oncology

Background:

  • Cancer's global mortality impact necessitates innovative therapeutic strategies.
  • Kinase signaling pathways are crucial in cancer initiation and progression.
  • Targeted therapy using small molecules offers a promising approach to inhibit kinase activity.

Purpose of the Study:

  • To review the historical development (1999-2023) of Small Molecule Kinase Inhibitors (SMKIs).
  • To explore the application and design of hydantoin, thiazolidinedione, and rhodanine derivatives as kinase inhibitors.
  • To summarize structural information for enhancing future kinase inhibitor development.

Main Methods:

  • Literature review of SMKIs discovery and development.
  • Analysis of structure-activity relationships for specific kinase inhibitor subclasses.
  • Compilation of molecular interaction data for derivative design.

Main Results:

  • Overview of SMKI evolution and molecular perspectives.
  • Detailed examination of hydantoin, thiazolidinedione, and rhodanine derivatives targeting EGFR, PI3K, VEGFR, Pim, c-Met, CDK, IGFR, and ERK.
  • Identification of key structural features influencing kinase inhibition potency.

Conclusions:

  • SMKIs represent a significant advancement in targeted cancer therapy.
  • Hydantoin, thiazolidinedione, and rhodanine scaffolds show potential for developing potent kinase inhibitors.
  • Further research into structure-activity relationships can optimize future SMKI design for improved efficacy.

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