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Eur J Med Chem ; 140: 1-19, 2017 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-28918096

RESUMO

Aurora kinase belongs to serine/threonine kinase family which controls cell division. Therapeutic inhibition of Aurora kinase showed great promise as probable anticancer regime because of its important role during cell division. Here, in this review, we have carried out exhaustive study of various synthetic molecules reported as Aurora kinase inhibitors and developed as lead molecule at various stages of clinical trials from its discovery in 1995 to till date. We reported details of small molecules, specifically inhibiting all 3 types of Aurora kinases, which includes extensive literature search in various database like various scientific journals, patents, scifinder and PubMed database, internet resources, books, etc. IC50 values of tumor growth inhibition, in-vitro and in-vivo activity along with clinical trial data. Here, we took efforts to describe essence of Aurora kinase and its inhibition which could be used to develop anti-mitotic drug for the treatment of cancer. In conclusion, we also discuss future perspectives for development of novel inhibitors and their scope in drug development process.


Assuntos
Antineoplásicos/farmacologia , Aurora Quinases/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Bibliotecas de Moléculas Pequenas/farmacologia , Animais , Antineoplásicos/química , Aurora Quinases/metabolismo , Proliferação de Células/efeitos dos fármacos , Ensaios Clínicos como Assunto , Humanos , Estrutura Molecular , Inibidores de Proteínas Quinases/química , Bibliotecas de Moléculas Pequenas/química
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