Derivatives of 4-(1H-pyrazol-4-yl)pyrimidine CDK2 inhibitors as potential anticancer agents : design, synthesis & evaluation /

dc.contributor.authorFanta, Biruk Sintayehu
dc.contributor.schoolUniversity of South Australia. UniSA Clinical and Health Sciences
dc.contributor.schoolUniSA Clinical and Health Sciences
dc.date.issued2022
dc.description1 ethesis (xv, 181 pages) :
dc.descriptioncolour illustrations, colour charts.
dc.descriptionIncludes bibliographical references (pages 170-197)
dc.description.abstractCyclin dependent kinase 2 (CDK2) is a serine/threonine protein kinase that plays an important role in regulating various facets of the cell division cycle. Deregulation of CDK2 and its activating partners is associated with a myriad of human tumours and resistance to anticancer drugs. Thus, CDK2 has become an attractive target for the development of new anticancer therapies. This research aimed to identify potent and selective CDK2 inhibitors which have the potential to be developed as anticancer drugs. Specifically, the thesis reported the design, synthesis and evaluation of the structures, biological activities and structure-activity-relationships of novel derivatives of 4-(1H-pyrazol-4-yl)pyrimidine. Furthermore, the antiproliferative mechanisms of the lead compounds were described and the discovery of a first-in-class, potent and highly selective CDK5 inhibitor was reported.
dc.description.dissertationThesis (PhD(Medical Science))--University of South Australia, 2022.
dc.identifier.urihttps://hdl.handle.net/11541.2/30305
dc.language.isoen
dc.provenanceCopyright 2022 Biruk Sintayehu Fanta.
dc.subjectCDK2;anticancer;bioioster;CDK2 inhibitor
dc.subject.lcshCancer
dc.subject.lcshCyclin-dependent kinases
dc.subject.lcshNucleic acids
dc.titleDerivatives of 4-(1H-pyrazol-4-yl)pyrimidine CDK2 inhibitors as potential anticancer agents : design, synthesis & evaluation /
dc.typethesis
dcterms.accessRights506 0#$fstar $2Unrestricted online access
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ror.mmsid9916675530901831

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