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Open AccessExtended Abstract

Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors

School of Chemical Sciences, University of Auckland, Auckland 1142, New Zealand
Auckland Cancer Society Research Centre, University of Auckland, Grafton, Auckland 1023, New Zealand
Author to whom correspondence should be addressed.
Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, Barcelona, Spain, 15–17 May 2019.
Proceedings 2019, 22(1), 67;
Published: 12 August 2019
(This article belongs to the Proceedings of The Molecules Medicinal Chemistry Symposium)
PDF [129 KB, uploaded 12 August 2019]


The phosphatidyl–choline-specific phospholipase C (PC-PLC) enzyme has been shown to be an important enzyme involved in various cell-signaling processes. Furthermore, PC-PLC has been shown to be upregulated in various cancer cell lines, thereby presenting itself as a potential anti-cancer therapeutic target. Current PC-PLC inhibitors, including the literature standard inhibitor D609 possess characteristics making them unsuitable for clinical use. We have discovered a new class of potent PC-PLC inhibitors with much improved activity and drug-like properties than D609. The synthesis and SAR study of this class of active compounds is presented.
Keywords: PC-PLC; SAR study; enzyme inhibition; phospholipase C PC-PLC; SAR study; enzyme inhibition; phospholipase C
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Pilkington, L.I.; Leung, E.; Barker, D. Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors. Proceedings 2019, 22, 67.

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