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Related Experiment Video

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Facile Preparation of 4-Substituted Quinazoline Derivatives

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Published on: February 15, 2016

Quinol derivatives as potential trypanocidal agents.

Amy Capes¹, Stephen Patterson, Susan Wyllie

¹Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Dundee DD1 5EH, UK.

Bioorganic & Medicinal Chemistry

|January 24, 2012

Summary

Researchers explored quinols as anti-cancer agents and for treating African trypanosomiasis. While modified quinols showed improved selectivity against the parasite Trypanosoma brucei, their potency was reduced.

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Area of Science:

Medicinal Chemistry
Parasitology
Drug Discovery

Background:

Quinols are investigated as potential anti-cancer agents due to their mechanism as double Michael acceptors.
Quinols exhibit activity against Trypanosoma brucei, the parasite causing human African trypanosomiasis.
Initial quinol screens showed limited selectivity against mammalian MRC5 cells.

Purpose of the Study:

To screen additional quinol compounds against Trypanosoma brucei.
To develop structure-activity relationships (SAR) for quinols targeting T. brucei.
To enhance the selectivity of quinols against T. brucei by incorporating parasite-specific transporter motifs.

Main Methods:

Screening of novel quinol derivatives against T. brucei.
Derivation of structure-activity relationships (SAR) for quinol compounds.
Synthesis and evaluation of quinols functionalized with melamine and benzamidine moieties.

Main Results:

Further quinol screening confirmed activity against T. brucei but maintained low selectivity over MRC5 cells.
Structure-activity relationships were established for the quinol series.
Transporter motif-containing quinol analogues demonstrated improved selectivity but decreased potency against T. brucei.

Conclusions:

Incorporating melamine and benzamidine motifs can increase quinol selectivity for T. brucei.
Further optimization is required to balance potency and selectivity in developing quinol-based therapeutics for African trypanosomiasis.