Session: Posters:

Human African trypanosomiasis (HAT,or sleeping sickness) is a parasitic disease caused by two subspecies of Trypanosoma brucei that is life threatening if left untreated. Existing therapies for this disease possess severe drawbacks such as high toxicity and inconvenient dosing regimens. In continuation of our drug development program for trypanosomiasis by utilizing lead repurposing, we have identified the 2,4-disubstituted pyrimidine hit AZD-5438, a pan-CDK inhibitor that inhibits T. brucei cell growth with nanomolar potency in in vitro studies. Results from current efforts in exploration of structure-activity and structure-property relationships will be reported, working towards a potent lead compound with improved selectivity and ADME properties.

Rosario Diaz-Gonzalez

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