Logo image
The first two cantharidin analogues displaying PP1 selectivity
Journal article   Peer reviewed

The first two cantharidin analogues displaying PP1 selectivity

A McCluskey, M A Keane, C C Walkom, M C Bowyer, A T R Sim, David James Young and J A Sakoff
Bioorganic & Medicinal Chemistry Letters, Vol.12(3), pp.391-393
2002
url
https://doi.org/10.1016/S0960-894X(01)00777-6View
Published Version

Abstract

cantharidin ester derivative furan maleic acid maleimide phosphoprotein phosphatase 1 phosphoprotein phosphatase 2A thiophene
High pressure Diels-Alder reactions of furan and dimethylmaleate, and thiophene and maleimide resulted in two cantharidin analogues, 3 and 6 possessing PP1 selectivity (>40- and >30-fold selectivity) over PP2A. Both compounds exhibited moderate PP1 activity, 3 IC50 50 μM and 6 IC50 12.5 μM. Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity. © 2002 Elsevier Science Ltd. All rights reserved.

Details

Metrics

InCites Highlights

These are selected metrics from InCites Benchmarking & Analytics tool, related to this output

Collaboration types
Domestic collaboration
Web Of Science research areas
Chemistry, Medicinal
Chemistry, Organic

UN Sustainable Development Goals (SDGs)

This output has contributed to the advancement of the following goals:

#3 Good Health and Well-Being

Source: InCites

Logo image