Quinazoline and quinazolinone as important medicinal scaffolds: a comparative patent review (2011–2016)

ABSTRACT

Introduction: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. A variety of marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities.

Area covered: This review covers recent efforts in the synthesis and biological screening of quinazoline/quinazolinone based compounds from 2011–2016.

Expert opinion: Quinazoline and quinazolinones represent a diverse class of biologically active nitrogen heterocyclic compounds with immense therapeutic potential. Their ease of synthetic accessibility, and flexibility in structural modifications and functionalization further adds to their appeal in medicinal chemistry. A number of currently available drugs are based on quinazoline/quinazolinone scaffold. It is interesting to note that, among the recent patents available, a lot of them focus on the promising anticancer activity of quinazoline and quinazolinone containing compounds. However their biological activity is certainly not limited to anticancer only, they are also known to elicit a number of other biological and physiological effects in vitro and in vivo respectively. The interest in quinazolines and quinazolinones is ever growing, since they offer a fairly diverse chemical space for exploration of medicinal potential.

KEYWORDS:

• Quinazoline
• quinazolinone
• biological activities
• heterocyclic compounds

Article highlights

1. Quinazoline/quinazolinone-based compounds occupy a unique place in medicinal chemistry.

2. Several different drugs contain quinazoline /quinazolinone scaffolds.

3. The review covers the recent progress (2011–2016) toward the synthesis and biological evaluation of quinazoline/quinazolinone derivatives.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties. Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

Higher Education Commission (HEC) Pakistan (Project Number 20-1910) under National Research Program for Universities is gratefully acknowledged for financial support.