An appraisal of anticancer activity with structure–activity relationship of quinazoline and quinazolinone analogues through EGFR and VEGFR inhibition: A review

Abstract

Cancer is one of the leading causes of death. Globally a huge number of deaths and new incidences are reported annually. Heterocyclic compounds have been proved to be very effective in the treatment of different types of cancer. Among different heterocyclic scaffolds, quinazoline and quinazolinone core were found versatile and interesting with many biological activities. In the discovery of novel anticancer agents, the Quinazoline core is very effective. The FDA has approved more than 20 drugs as an anticancer bearing quinazoline or quinazolinone core in the last two decades. One prime example is Dacomitinib, which was newly approved for non-small-cell lung carcinoma treatment in 2018. These drugs work by different pathways to prevent the spread of cancer cell progression, including inhibition of different kinases, tubulin, kinesin spindle protein, and so forth. This review presented recent developments of quinazoline/quinazolinone scaffold bearing derivatives as anticancer agents acting as epidermal growth factor receptor (EGFR) vascular endothelial growth factor receptor (VEGFR), and dual EGFR/VEGFR inhibitors.

[Cell@Al2O3(HEPiPY)]DCA: A Cellulose Supported Ionic Liquid Catalyst for Synthesis of 11 b,12‐dihydro‐6H,13Hbenzo[5,6][1,3]oxazino[3,4‐a]quinazoline‐6,13‐dione along with in silico assessments

“…VEGFR-2 is an important enzyme in the living systems with hazardous effects in an overexpression state; hence, considerable efforts have been focused on the exploration of novel ligand inhibitors against the VEGFR-2 overactivity up to now. [32][33][34] To this aim, the electronic structure features of oxazinoquinazolines (3a-i) derivatives were first analyzed regarding the stabilizations and features evaluations of 3D molecular models. In this step, the B3LYP/6-31G* level of density functional theory (DFT) calculations were carried out using the Gaussian program.…”

Synthesis, Characterization, Molecular Docking and in vitro Biological Studies of Thiazolidin‐4‐one Derivatives as Anti‐Breast‐Cancer Agents

“…Overexpression of VEGFR1 has been associated with a poor prognosis, as it is thought to contribute to tumor growth and metastasis. [11] Thiazolidin-4-one and its derivatives have a wide range of pharmacological activities such as anticancer [12][13][14][15][16][17] anti-inflammatory, analgesic, anticonvulsant, antimicrobial, local and spinal anesthetics, central nervous system stimulants, hypnotics, anti-HIV, antidiabetic, follicle-stimulating hormone receptor antagonist. [18][19][20][21][22] The aim of this study is to develop new and effective anticancer agents through the synthesis of thiazolidin-4-one derivatives of 4-furfuryloxy-benzohydrazide.…”

“…VEGFR1 has been found to be overexpressed in many types of cancer, including breast, ovarian, lung, and prostate cancer. Overexpression of VEGFR1 has been associated with a poor prognosis, as it is thought to contribute to tumor growth and metastasis [11] …”

Assembly of iodinated indolo[1,2-c]quinazoline amines via I2/CHP-promoted cascade annulation of isocyanides and diarylalkynes

“…The indolo[1,2- c ]quinazoline 1 scaffolds are a class of poly-fused heterocyclic compounds that have attracted more and more attention as biologically active natural products 2 and compounds with pharmaceutical applications. 3 For example, the marine alkaloid hinckdentine A (Fig. 1, I ) contains biologically active dihydrotryptamine and dihydropyrimidine units, 4 which have important value in drug development.…”