Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors

Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis. Aurora-A kinase is overexpressed in many malignant solid tumors, such as breast, ovarian, col...

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Detalles Bibliográficos
Autor principal: Abdullah, Omeima
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8469531/
https://www.ncbi.nlm.nih.gov/pubmed/34577149
http://dx.doi.org/10.3390/molecules26185678
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author Abdullah, Omeima
author_facet Abdullah, Omeima
author_sort Abdullah, Omeima
collection PubMed
description Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis. Aurora-A kinase is overexpressed in many malignant solid tumors, such as breast, ovarian, colon, and pancreatic cancers. Thus, inhibiting Aurora-A kinase activity is a promising approach for cancer treatment. Here, new triazole derivatives were designed as bioisosteric analogues of the known inhibitor JNJ-7706621. The new compounds showed interesting inhibitory activity against Aurora-A kinase, as attested by IC(50)s in the low to submicromolar range.
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spelling pubmed-84695312021-09-27 Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors Abdullah, Omeima Molecules Communication Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis. Aurora-A kinase is overexpressed in many malignant solid tumors, such as breast, ovarian, colon, and pancreatic cancers. Thus, inhibiting Aurora-A kinase activity is a promising approach for cancer treatment. Here, new triazole derivatives were designed as bioisosteric analogues of the known inhibitor JNJ-7706621. The new compounds showed interesting inhibitory activity against Aurora-A kinase, as attested by IC(50)s in the low to submicromolar range. MDPI 2021-09-18 /pmc/articles/PMC8469531/ /pubmed/34577149 http://dx.doi.org/10.3390/molecules26185678 Text en © 2021 by the author. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Abdullah, Omeima
Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
title Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
title_full Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
title_fullStr Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
title_full_unstemmed Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
title_short Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors
title_sort design, synthesis, and biochemical evaluation of new triazole derivatives as aurora-a kinase inhibitors
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8469531/
https://www.ncbi.nlm.nih.gov/pubmed/34577149
http://dx.doi.org/10.3390/molecules26185678
work_keys_str_mv AT abdullahomeima designsynthesisandbiochemicalevaluationofnewtriazolederivativesasauroraakinaseinhibitors

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