SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME 2-ARYLBENZOXAZOLE ACETIC ACID DERIVATIVES AS PROMISING ANTICANCER AGENTS

被引：3

作者：

Jilani, Jamal Abdellatif ^{[1
]}

Abualassal, Qais Ibrahim ^{[2
]}

Assaf, Areej Mashour ^{[3
]}

Abu Shmies, Reham Mahmoud ^{[4
]}

机构：

[1] Jordan Univ Sci & Technol, Fac Pharm, Dept Med Chem & Pharmacognosy, Irbid, Jordan

[2] Isra Univ, Fac Pharm, Dept Appl Pharmaceut Sci, Amman, Jordan

[3] Univ Jordan, Fac Pharm, Dept Biopharmaceut & Clin Pharm, Amman, Jordan

[4] Al Balqa Appl Univ, Fac Sci, Dept Chem, Al Salt, Jordan

来源：

ACTA POLONIAE PHARMACEUTICA | 2020年 / 77卷 / 05期

关键词：

cytotoxicity; arylbenzoxazoles; MCF-7; structure-activity relationships; lead tetraacetate; HETEROCYCLIC-COMPOUNDS; BENZIMIDAZOLES; BENZOXAZOLES;

D O I：

10.32383/appdr/127998

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The synthesis of a series of 2-arylbenzoxazole compounds possessing a cytotoxic activity as potential anticancer agents was achieved. Oxidative coupling of benzaldehyde with o-aminophenol utilizing lead tetraacelate approach was used to realize the synthesis of compounds 1-11. The cytotoxicity of 1-11 was screened against breast cancer cell line MCF-7 and human colon cancer cell line HCT-116 utilizing doxorubicin as a reference drug. Among these compounds, 2-(3-benzyloxyphenyl)benzoxazole-5-acetic acid (5) and 2-(4-methoxyphenyl)benzoxazol-5-acetic acid (10), were found to be promising cytotoxic compounds against the MCF-7 cell line. In addition, this study showed that the presence of an acetic acid group at position 5 of the benzoxazole nucleus enhances the activity. Moreover, we noticed that the presence of an oxygen atom directly linked to the phenyl substituent improves activity as well. These results offer a new benzoxazole based template to design and develop novel antineoplastic agents.

引用

页码：717 / 723

页数：7

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