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.

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.

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
4.7K
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists01:29

Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists

Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
Phenothiazines, such as prochlorperazine...
261
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.0K
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
194
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
2.0K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.5K