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Synthesis, characterization and biological evaluation of some 2-arylbenzoxazole acetic acid derivatives as potential anticancer agents

By: Jilani, Jamal Abdellatif.
Contributor(s): Qais Ibrahim Abualassal.
Publisher: New Delhi CSIR 2021Edition: Vol.60(B), Nov.Description: 1496-1501p.Subject(s): GENERAL CHEMISTRYOnline resources: Click here In: Indian journal of chemistry (Section B)Summary: A series of 2-arylbenzoxazole compounds possessing a cytotoxic activity as potential anticancer agents has been synthesised. Oxidative coupling of benzaldehyde with o-aminophenol utilizing lead tetraacetate approach has been used to realize the synthesis of compounds 1-11. The cytotoxicity of 1-11 have been screened against breast cancer cell line MCF-7 and human colon cancer cell line HCT-116 utilizing doxorubicin as reference drug. Among these compounds, 2-(3- benzyloxyphenyl)benzoxazole-5-acetic acid 5 and 2-(4-methoxyphenyl)benzoxazol-5-acetic acid 10, are found to be promising cytotoxic compounds against MCF-7 cell line. In addition, this study shows that the presence of acetic acid group at position 5 of benzoxazole nucleus enhances the activity. Moreover, it is noticed that the presence of oxygen atom directly linked to the phenyl substituent improves activity. The results offer a new benzoxazole based template to design and develop novel antineoplastic agents.
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A series of 2-arylbenzoxazole compounds possessing a cytotoxic activity as potential anticancer agents has been
synthesised. Oxidative coupling of benzaldehyde with o-aminophenol utilizing lead tetraacetate approach has been used to
realize the synthesis of compounds 1-11. The cytotoxicity of 1-11 have been screened against breast cancer cell line MCF-7 and
human colon cancer cell line HCT-116 utilizing doxorubicin as reference drug. Among these compounds, 2-(3-
benzyloxyphenyl)benzoxazole-5-acetic acid 5 and 2-(4-methoxyphenyl)benzoxazol-5-acetic acid 10, are found to be promising
cytotoxic compounds against MCF-7 cell line. In addition, this study shows that the presence of acetic acid group at position 5
of benzoxazole nucleus enhances the activity. Moreover, it is noticed that the presence of oxygen atom directly linked to the
phenyl substituent improves activity. The results offer a new benzoxazole based template to design and develop novel
antineoplastic agents.

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