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Updated: Jun 24, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Insight in Quinazoline-based HDAC Inhibitors as Anti-cancer Agents
Elena Martino1, Shruti Thakur2, Arun Kumar2
1Department of Science and Drug Technology, University of Turin, via Pietro Giuria 9, Turin, 10125, Italy.
Abstract:
Cancer remains a primary cause of death globally, and effective treatments are still limited. While chemotherapy has notably enhanced survival rates, it brings about numerous side effects. Consequently, the ongoing challenge persists in developing potent anti-cancer agents with minimal toxicity. The versatile nature of the quinazoline moiety has positioned it as a pivotal component in the development of various antitumor agents, showcasing its promising role in innovative cancer therapeutics. This concise review aims to reveal the potential of quinazolines in creating anticancer medications that target histone deacetylases (HDACs).
Insights
Quinazolines show promise as novel anticancer drugs targeting histone deacetylases (HDACs). This review explores their potential to create effective cancer treatments with fewer side effects than traditional chemotherapy.
Area of Science:
- Medicinal Chemistry
- Oncology
- Pharmacology
Background:
- Cancer is a leading global cause of death with limited effective treatments.
- Chemotherapy improves survival but causes significant side effects.
- Developing potent anticancer agents with minimal toxicity remains a critical challenge.
Purpose of the Study:
- To review the potential of quinazoline derivatives in developing novel anticancer therapeutics.
- To explore quinazolines as inhibitors of histone deacetylases (HDACs) for cancer treatment.
Main Methods:
- Literature review of existing studies on quinazoline-based anticancer agents.
- Analysis of structure-activity relationships of quinazolines targeting HDACs.
- Discussion of the therapeutic potential and challenges of quinazoline-HDAC inhibitors.
Main Results:
- Quinazoline scaffolds are versatile and have been incorporated into various antitumor agents.
- Several quinazoline derivatives exhibit potent anticancer activity by inhibiting HDACs.
- These compounds offer a promising avenue for targeted cancer therapy.
Conclusions:
- Quinazolines represent a valuable class of compounds for the development of next-generation anticancer drugs.
- Targeting HDACs with quinazoline-based inhibitors is a viable strategy to combat cancer.
- Further research is warranted to optimize these agents for clinical application.
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