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Synthesis and Characteristics of Metastable 2‐Benzyl‐4H‐3,1‐benzoxazin‐4‐one as Anticancer Agent and its Comparison with other Heterocyclic Compounds

Heterocyclic compounds with different heterocycle moieties, namely benzoxazinone, benzimidazole, quinazolinone, and benzofuranone heterocyclic rings, were synthesized, characterized and evaluated for their anticancer activities against Lung cancer cell line (A549) using Sulforhodamine B (SRB) assay....

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Published in:ChemistrySelect (Weinheim) 2019-12, Vol.4 (48), p.14056-14062
Main Authors: Mokhtar Radwan, Tasneem, Abdel‐Aziz El‐Hashash, Maher, Abdel‐Hamid Farouk Wasfy, Ashraf, Abdelhalim Abdallah, Suzan
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container_title ChemistrySelect (Weinheim)
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creator Mokhtar Radwan, Tasneem
Abdel‐Aziz El‐Hashash, Maher
Abdel‐Hamid Farouk Wasfy, Ashraf
Abdelhalim Abdallah, Suzan
description Heterocyclic compounds with different heterocycle moieties, namely benzoxazinone, benzimidazole, quinazolinone, and benzofuranone heterocyclic rings, were synthesized, characterized and evaluated for their anticancer activities against Lung cancer cell line (A549) using Sulforhodamine B (SRB) assay. In vitro, a compound with benzoxazinone scaffold namely 2‐benzyl‐3,1‐benzoxazin‐4‐one was shown to have the best antiproliferative activity against Lung cancer cell line (A549) with IC50 values 53.9 μM in comparison with other heterocyclic rings. This compound showed an excellent cytotoxicity effect against the pancreatic cancer cell line (PANC‐1) with IC50 values 0.15 μM, while it has a slight effect on the hepatocellular carcinoma cell line (HepG2). The 2‐benzyl‐3,1‐benzoxazin‐4‐one 1 exhibits good antiproliferative activity against Lung cancer cell line (A549) with IC50 values 53.9 μM and showed cytotoxicity effect against the pancreatic cancer cell line (PANC‐1) with IC50 values 0.15 μM.
doi_str_mv 10.1002/slct.201902773
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subjects Benzimidazole
Benzofuranone
Benzoxazinone
Quinazolinone
Sulforhodamine B
title Synthesis and Characteristics of Metastable 2‐Benzyl‐4H‐3,1‐benzoxazin‐4‐one as Anticancer Agent and its Comparison with other Heterocyclic Compounds
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