Journal article
Discovery of novel phosphatidylcholine-specific phospholipase C drug-like inhibitors as potential anticancer agents
C Eurtivong, LI Pilkington, M van Rensburg, RM White, HK Brar, S Rees, EK Paulin, CS Xu, N Sharma, IKH Leung, E Leung, D Barker, J Reynisson
European Journal of Medicinal Chemistry | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | Published : 2020
Abstract
Phosphatidylcholine–specific phospholipase C (PC-PLC) is a promising target for new anticancer treatment. Herein, we report our work in the discovery of novel drug-like PC-PLC inhibitors. Virtual screening led to the identification of promising hits from four different structural series that contain the molecular scaffold of benzenesulphonamides (10), pyrido[3,4-b]indoles (22), morpholinobenzoic acid (84) and benzamidobenzoic acid (80). 164 structural analogues were tested to investigate the chemical space around the hit series and to generate preliminary structurally activity relationships (SAR). Two of the pyrido[3,4-b]indoles (22_10 and 22_15) had comparable or better potency as D609, an ..
View full abstractGrants
Awarded by Health Research Council of New Zealand
Funding Acknowledgements
We are very grateful for the financial support from the Cancer Society of New Zealand (Ref: 17.01) and the Breast Cancer Partnership, Health Reseatch Council, New Zealand (Ref: 17/671).