Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols')

Cedric J Lion; Charles S Matthews; Geoffrey Wells; Tracey D Bradshaw; Malcolm F G Stevens; Andrew D Westwell

doi:10.1016/j.bmcl.2006.07.072

Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols')

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5005-8. doi: 10.1016/j.bmcl.2006.07.072.

Authors

Cedric J Lion¹, Charles S Matthews, Geoffrey Wells, Tracey D Bradshaw, Malcolm F G Stevens, Andrew D Westwell

Affiliation

¹ Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, UK.

PMID: 16908135
DOI: 10.1016/j.bmcl.2006.07.072

Abstract

The synthesis and in vitro antitumour evaluation of a new series of fluorinated benzothiazole-substituted 4-hydroxycyclohexa-2,5-dienones ('quinols') is described. The new compounds were found to be of comparable activity compared to the non-fluorinated precursor PMX 464, in terms of antiproliferative activity in sensitive human cancer cell lines (nanomolar GI(50) values) and inhibitory activity against the thioredoxin signalling system.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Cell Line, Tumor
Cell Proliferation / drug effects
Drug Screening Assays, Antitumor
Humans
Hydroquinones / chemical synthesis*
Hydroquinones / pharmacology
Signal Transduction / drug effects
Structure-Activity Relationship
Thioredoxins / metabolism

Substances

Antineoplastic Agents
Hydroquinones
Thioredoxins