The current landscape of quinazoline derivatives with in vivo anticancer therapeutic potential-part II

Shanshan Huang1, Zhi Xu1, Yan Zhang2

  • 1School of Chemistry and Pharmaceutical Engineering, Huanghuai University, Zhumadian, Henan, China.

PubMed

Insights

Quinazoline derivatives show promise as novel anticancer drugs, offering new therapeutic strategies to overcome drug resistance in cancer treatment. This review highlights their potential and mechanisms of action.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Pharmacology

Background:

  • Cancer remains a leading global cause of death, with drug resistance posing a significant challenge.
  • Multidrug resistance in cancer necessitates the development of novel chemotherapeutic agents.
  • Quinazoline derivatives are recognized for their diverse anticancer activities and established therapeutic roles.

Purpose of the Study:

  • To review the in vivo anticancer potential of quinazoline derivatives.
  • To explore the mechanisms of action, toxicity, and pharmacokinetics of these compounds.
  • To provide an updated overview of recent advancements in quinazoline-based cancer therapeutics.

Main Methods:

  • Comprehensive literature search for studies published from 2015 to the present.
  • Analysis of research focusing on quinazoline derivatives with demonstrated in vivo anticancer activity.
  • Evaluation of reported mechanisms, toxicity profiles, and pharmacokinetic data.

Main Results:

  • Quinazoline derivatives exhibit anticancer effects via cell cycle arrest, apoptosis induction, and autophagy modulation.
  • Several quinazoline-based agents have shown significant in vivo efficacy in preclinical models.
  • The review details the therapeutic potential, safety, and drug-like properties of various derivatives.

Conclusions:

  • Quinazoline derivatives represent a valuable class of compounds for developing next-generation anticancer therapies.
  • Understanding their mechanisms and properties is crucial for advancing their clinical application.
  • Continued research into quinazoline derivatives holds significant promise for overcoming cancer drug resistance.

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...
4.9K
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...
7.8K
Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
8.0K
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...
446
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
5.1K
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,...
322