University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh, 160014, India.
University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh, 160014, India.
Eur J Med Chem. 2021 Feb 5;211:113016. doi: 10.1016/j.ejmech.2020.113016. Epub 2020 Nov 12.
Presently cancer is a grave health issue with predominance beyond restrictions. It can affect any organ of the body. Most of the available chemotherapeutic drugs are highly toxic, not much selective and eventually lead to the development of resistance. Therefore, a target specific palliative approach for the treatment of cancer is required. Remarkable advancements in science have illuminated various molecular pathways responsible for cancer. This has resulted in abundant opportunities to develop targeted anticancer agents. Quinazoline nucleus is a privileged scaffold with significant diversified pharmacological activities. Numerous established anticancer quinazoline derivatives constitute a new class of chemotherapeutic agents which are found to act by inhibiting various protein kinases as well as other molecular targets. A recent update on various quinazoline derivatives acting on different types of molecular targets for the treatment of cancer has been compiled in this review. Brief SAR studies of quinazoline derivatives acting through different mechanisms of action have been highlighted. The comprehensive medicinal chemistry aspects of these agents in this review provide a panoramic view to the biologists as well as medicinal chemists working in this area and would assist them in their efforts to design and synthesize novel quinazoline based anticancer compounds.
目前，癌症是一个严重的健康问题，其普遍性超出了限制。它可以影响身体的任何器官。大多数现有的化疗药物毒性很高，选择性不强，最终会导致耐药性的产生。因此，需要一种针对癌症的靶向姑息治疗方法。科学的显著进步揭示了导致癌症的各种分子途径。这为开发靶向抗癌药物提供了丰富的机会。喹唑啉核是一种具有重要多样化药理活性的特权支架。许多已建立的抗癌喹唑啉衍生物构成了一类新的化疗药物，这些药物被发现通过抑制各种蛋白激酶以及其他分子靶点起作用。本综述综述了不同类型的分子靶点上作用于不同类型的分子靶点的各种喹唑啉衍生物。通过不同作用机制起作用的喹唑啉衍生物的简要 SAR 研究已经被强调。这些药物的全面药物化学方面为在该领域工作的生物学家和药物化学家提供了全景视图，并将帮助他们设计和合成基于喹唑啉的新型抗癌化合物。
