Synthesis and anticancer studies of novel benzimidazole/benzoxazole-pyrazine derivatives

A new series of aryl tethered benzimidazole-pyrazine and benzoxazole-pyrazine derivatives was synthesized via an intermediate chloro-aryl amine from 2,6-dichloropyrazine by adopting Pd(0)-catalysed Suzuki cross coupling and cyclo-condensation successively.The chloro-aryl amine was synthesised in high yield under transition metal free basic conditions.An efficient microwave mediated strategy was developed for the synthesis of benzoxazole-pyrazine derivatives.All the synthesized final targets were screened for in vitro cytotoxicity against human cancer cell lines MCF-7(breast), A-549(lung), A-375(melanoma) and DU-145(prostate) by employing Doxorubicin and Etoposide as controls.

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Publication Details

Journal
ARKIVOC
Published
2024-09-12
DOI
https://doi.org/10.24820/ark.5550190.p012.241
Primary Topic
Synthesis and biological activity
Type
article
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article

Synthesis and anticancer studies of novel benzimidazole/benzoxazole-pyrazine derivatives

Krishna Reddy Valluru, Umamaheswar Rao G, Jayaprakash Rao Yerrabelly, Hemasri Yerrabelly
ARKIVOC
Synthesis and biological activity
article

Synthesis and anticancer studies of novel benzimidazole/benzoxazole-pyrazine derivatives

Krishna Reddy Valluru, Umamaheswar Rao G, Jayaprakash Rao Yerrabelly, Hemasri Yerrabelly
article en

Abstract

A new series of aryl tethered benzimidazole-pyrazine and benzoxazole-pyrazine derivatives was synthesized via an intermediate chloro-aryl amine from 2,6-dichloropyrazine by adopting Pd(0)-catalysed Suzuki cross coupling and cyclo-condensation successively.The chloro-aryl amine was synthesised in high yield under transition metal free basic conditions.An efficient microwave mediated strategy was developed for the synthesis of benzoxazole-pyrazine derivatives.All the synthesized final targets were screened for in vitro cytotoxicity against human cancer cell lines MCF-7(breast), A-549(lung), A-375(melanoma) and DU-145(prostate) by employing Doxorubicin and Etoposide as controls.

ARKIVOCVol. 2024(8)
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Synthesis and biological activity
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