a H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences , University of Karachi , Karachi , Pakistan.
b Department of Chemistry , Forman Christian College (A Chartered University) , Lahore , Pakistan.
Expert Opin Ther Pat. 2018 Apr;28(4):281-297. doi: 10.1080/13543776.2018.1432596. Epub 2018 Feb 5.
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.
This review covers recent efforts in the synthesis and biological screening of quinazoline/quinazolinone based compounds from 2011-2016.
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.
喹唑啉和喹唑酮类骨架是一类重要的具有生物活性的含氮杂环化合物。许多市售药物都是基于这些部分。已经报道了具有喹唑啉/喹唑酮部分的多种分子具有广泛的生物活性。
本文综述了 2011 年至 2016 年期间基于喹唑啉/喹唑啉酮的化合物的合成和生物筛选的最新进展。
喹唑啉和喹唑酮代表了一类具有广泛生物活性的含氮杂环化合物,具有巨大的治疗潜力。它们易于合成、结构修饰和功能化的灵活性进一步增加了它们在药物化学中的吸引力。许多现有的药物都是基于喹唑啉/喹唑啉酮骨架。有趣的是,在现有的专利中,有很多专利都集中在喹唑啉和喹唑啉酮类化合物具有有前途的抗癌活性上。然而,它们的生物活性当然不仅限于抗癌,它们也被证明在体外和体内分别具有许多其他生物学和生理学作用。人们对喹唑啉和喹唑啉酮的兴趣日益浓厚,因为它们为探索药物潜力提供了相当多样化的化学空间。