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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Bibliographic Details
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
Format: Article
Language:English
Subjects:
Benzimidazole
Benzofuranone
Benzoxazinone
Quinazolinone
Sulforhodamine B
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Summary: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.
ISSN:2365-6549
2365-6549
DOI:10.1002/slct.201902773