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

Date

2022

Authors

Fanta, Biruk Sintayehu

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thesis

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Abstract

Cyclin 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.

School/Discipline

University of South Australia. UniSA Clinical and Health Sciences
UniSA Clinical and Health Sciences

Dissertation Note

Thesis (PhD(Medical Science))--University of South Australia, 2022.

Provenance

Copyright 2022 Biruk Sintayehu Fanta.

Description

1 ethesis (xv, 181 pages) :
colour illustrations, colour charts.
Includes bibliographical references (pages 170-197)

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506 0#$fstar $2Unrestricted online access

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