Harnessing the quinoline core for targeted cancer therapy

Area of Science:

• Medicinal Chemistry
• Oncology
• Drug Discovery

Background:

• The quinoline scaffold is a versatile framework in medicinal chemistry.
• Quinoline derivatives have demonstrated significant potential in targeted cancer treatment.
• Advances in synthetic chemistry enable the development of novel quinoline-based anticancer agents.

Purpose of the Study:

• To systematically review quinoline derivatives for targeted cancer therapy from 2017-2026.
• To analyze rational design, structure-activity relationships (SARs), and antitumor efficacy.
• To identify challenges and future directions for quinoline-based anticancer drug development.

Main Methods:

• Literature review of quinoline derivatives in cancer therapy.
• Categorization of compounds by major molecular target families (kinases, metabolic enzymes, epigenetic regulators, drug transporters).
• Emphasis on structure-activity relationships (SARs) and preclinical/clinical efficacy data.

Main Results:

• Summary of recent advances in quinoline derivatives targeting diverse molecular pathways in cancer.
• Identification of key SARs driving antitumor activity.
• Highlighting progress in rational design for improved efficacy.

Conclusions:

• Quinoline derivatives represent a promising class of anticancer agents.
• Challenges include isoform selectivity, pharmacokinetics, and drug resistance.
• Future strategies should involve dual-targeting and prodrug approaches for next-generation therapies.