A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies

被引：143

作者：

Borisa, Ankit C. ^{[1
]}

Bhatt, Hardik G. ^{[1
]}

机构：

[1] Nirma Univ, Inst Pharm, Dept Phannaceut Chem, Ahmadabad 382481, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 140卷

关键词：

Aurora kinase; Aurora-A; Aurora-B; Aurora-C; INCENP; Small molecule inhibitors; CANCER-CELL-LINES; SUPPRESSES TUMOR-GROWTH; A KINASE; POTENT AURORA; IN-VIVO; SELECTIVE AURORA; B-KINASE; ANTITUMOR-ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; PYRIMIDINE-DERIVATIVES;

D O I：

10.1016/j.ejmech.2017.08.045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2017 Elsevier Masson SAS. All rights reserved.

引用

页码：1 / 19

页数：19

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