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Updated: May 9, 2026
A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
Published on: March 10, 2017
Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part
Yassir Younis1, Leslie J Street, David Waterson
1Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
Abstract:
In the second part of this Miniperspectives series, we highlight our medicinal chemistry efforts involving progression of hits from whole cell high-throughput screening (HTS) of a SoftFocus kinase library against the malaria parasite Plasmodium falciparum . Successful SAR exploration in Hit-to-Lead and Lead Optimization efforts leading to the selection of a preclinical development candidate are demonstrated. Related efforts by researchers from Broad/Genzyme, Anacor, and GSK are briefly covered.
