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Updated: Nov 21, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Exploring Quinolone Scaffold: Unravelling the Chemistry of Anticancer Drug Design
Vishal Sharma1, Rina Das1, Dinesh Kumar Mehta1
1MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Hr 133207, India.
Abstract:
Globally, cancer is considered as the major leading cause in burdening the patient's health care system globally. The growing threat of drug-resistant cancers renders an urgent need to develop more successful candidates for the anti-cancer therapy. In view of the outstanding pharmacological activities, Quinolone and its derivatives have attracted more attention towards drug designing and biological evaluation in the search for new drug molecules. The inspired researchers attempted efforts in order to discover the quinolone based analogs due to their wide range of biological activities. Due to immense pharmacological importance, distinct synthetic methods have been executed to attain new drug entities from quinolones and all the reported molecules have shown constructive anticancer activities. Some of the synthetic protocols like one pot synthesis, post-Ugi-transformation, catalysed based synthesis, enzyme-based synthesis and nano-catalyst based synthetic procedures are also discussed as recent advancements in the production of quinolone derivatives. In this review, recent synthetic approaches in the medicinal chemistry of quinolones and potent quinolone derivatives on the basis of structural activity relationship are outlined. Moreover, their major methods and modifications are discussed.
Insights
This review highlights quinolone derivatives as promising anti-cancer agents. Recent synthetic methods and structure-activity relationships are discussed for developing new drug candidates against resistant cancers.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Organic Synthesis
Background:
- Cancer poses a significant global health burden, exacerbated by increasing drug resistance.
- Quinolone derivatives exhibit notable pharmacological activities, making them attractive for anti-cancer drug development.
Purpose of the Study:
- To review recent synthetic approaches for quinolone derivatives.
- To outline potent quinolone derivatives based on structure-activity relationships.
- To discuss advancements in the synthesis of novel anti-cancer drug candidates.
Main Methods:
- Exploration of diverse synthetic strategies including one-pot synthesis, post-Ugi-transformation, and catalyst-based methods.
- Analysis of structure-activity relationships for quinolone derivatives.
- Review of recent literature on quinolone-based anti-cancer agents.
Main Results:
- Various synthetic protocols have been successfully employed to generate quinolone derivatives.
- Reported quinolone molecules demonstrate significant anti-cancer activities.
- Recent advancements include enzyme-based and nano-catalyst based synthetic procedures.
Conclusions:
- Quinolone derivatives represent a vital class of compounds for developing novel anti-cancer therapies.
- Continued research into synthetic modifications and structure-activity relationships is crucial for optimizing anti-cancer efficacy.
- The development of efficient and innovative synthetic methods is key to advancing quinolone-based drug discovery.
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