1. Academic Validation
  2. The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton

The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton

  • Bioorg Med Chem. 2019 Feb 1;27(3):568-577. doi: 10.1016/j.bmc.2018.12.032.
Yang Li 1 Jie Xiao 1 Qizhi Zhang 1 Wenmei Yu 1 Mengqin Liu 2 Yu Guo 1 Jun He 3 Yunmei Liu 1
Affiliations

Affiliations

  • 1 Institute of Pharmacy & Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China.
  • 2 Institute of Chemistry and Materials Science, Hengyang Normal University, Hengyang 421001, China.
  • 3 Institute of Chemistry & Chemical Engineering, University of South China, Hengyang 421001, China. Electronic address: hjhsm@126.com.
Abstract

Quinazoline was originally utilized as an anti-tumor treatment, and its various derivatives can be directly extracted from Plants. In recent years, protein kinases (PK) have been well recognized in the development of tumor drugs. Functionally, PK serves a vital role in the Apoptosis, proliferation, differentiation, migration and cell cycle of tumor cells. Due to its good physicochemical properties, quinazoline skeleton, a superior type of PK inhibitor, has been extensively used in anti-tumor drug design. An increasing number of studies on quinazoline synthesis have been reported and used by different groups to effectively develop novel derivatives. Thus, several studies have been approved for the use of quinazoline derivatives as inhibitors of Other kinases, including Src and histone deacetylase. The aim of the present review was to summarize the mechanism of quinazoline compounds as PK inhibitors, their biological structure-activity relationship such as the substituted quinazoline compounds with different functional groups in the apoptotic process, and their effect on the proliferation of tumor cells. The development of novel agents based on the antitumor functions of quinazoline molecular compounds may improve the clinical outcomes of the affected population, particularly in patients with Cancer.

Keywords

Anti-tumor; Drug target; Inhibitors of protein kinases; Quinazoline derivatives; Structure-activity relationship.

Figures