Discovery of novel cyclin-dependent kinase 8 inhibitors as potential antitumour agents /
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(Published version)
Date
2019
Authors
Philip, Stephen
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thesis
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Abstract
CDK8, a member of the CDK family has recently been identified as a key oncogenic driver in many cancers. This dissertation describes the design, synthesis, and biological evaluation of novel series of 1-phenyl-3-(5-(pyrimidin-4-yl)thiazol-2-yl)urea derivatives as CDK8 inhibitors for the treatment of cancer. To identify potent and selective CDK8 inhibitors, we used a hybrid-design approach, and synthesised over 60 novel molecules where various positions of the 1-phenyl-3-(5-(pyrimidin-4-yl)thiazol-2-yl)urea scaffold were modified. The lead compound thus identified holds significant promise as a preclinical drug candidate and as a biochemical tool to dissect the complex role of CDK8 in cancers.
School/Discipline
University of South Australia. School of Pharmacy and Medical Sciences.
School of Pharmacy and Medical Sciences
School of Pharmacy and Medical Sciences
Dissertation Note
Thesis (PhD(Pharmaceutical Science))--University of South Australia, 2019.
Provenance
Copyright 2019 Stephen Philip.
Description
1 ethesis (xx, 198 pages) :
illustrations (some colour), charts (some colour)
Includes bibliographical references (pages 173-191)
illustrations (some colour), charts (some colour)
Includes bibliographical references (pages 173-191)
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506 0#$fstar $2Unrestricted online access