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

摘要

Abstract 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. IC 50 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. Graphical abstract Display Omitted Highlights ? Aurora kinase has emerged as one of the important cell cycle regulator in cancer genesis. ? Its inhibition can prove as an effective anti-mitotic treatment. ? Kinase inhibitors involving small molecules have been found as useful strategy. ? Advance clinical/preclinical candidates are studied and summarised with detailed activity profile. ? Multi kinase inhibition, ATP-competitive inhibition and combination therapy are novel approaches for cancer treatment.