Monash University

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Reason: Under embargo until July 2021. After this date a copy can be supplied under Section 51(2) of the Australian Copyright Act 1968 by submitting a document delivery request through your library

The Development of HIV-1 Integrase Allosteric Inhibitors Using a Fragment Based Drug Discovery Approach

posted on 2018-07-15, 09:07 authored by DAN ZHENG
HIV-1 integrase (IN) is an enzyme that is essential for viral replication. Previous work within our group identified a molecule as a hit that bound to IN and had potential to be developed as an inhibitor of HIV. This thesis describes the hit-to-lead optimisation process of developing the hit into a high-affinity lead compound using a Fragment-Based Drug Discovery approach. Overall, in this work 99 analogues were synthesised and evaluated using multiple assays. The binding affinity of the hit was improved by a factor of 700 thousand.


Campus location


Principal supervisor

David Chalmers

Additional supervisor 1

Martin Scanlon

Additional supervisor 2

Jamie Simpson

Year of Award


Department, School or Centre

Medicinal Chemistry

Additional Institution or Organisation



Doctor of Philosophy

Degree Type



Faculty of Pharmacy and Pharmaceutical Sciences