Identification of small-molecule inhibitors of Trypansoma cruzi replication.

Bioorg Med Chem Lett

Authors	Andrew Germain Leigh Carmody Chris Dockendorff Cristina Galan-Rodriguez Ana Rodriguez Stephen Johnston Joshua Bittker Lawrence MacPherson Sivaraman Dandapani Michelle Palmer Stuart Schreiber Benito Munoz
Keywords	Structure-Activity Relationship Small Molecule Libraries Molecular Structure Inhibitory Concentration 50 Trypanocidal Agents Trypanosoma cruzi
Abstract	We report the outcome of a high-throughput small-molecule screen to identify novel, nontoxic, inhibitors of Trypansoma cruzi, as potential starting points for therapeutics to treat for both the acute and chronic stages of Chagas disease. Two compounds were identified that displayed nanomolar inhibition of T. cruzi and an absence of activity against host cells at the highest tested dose. These compounds have been registered with NIH Molecular Libraries Program (probes ML157 and ML158).
Year of Publication	2011
Journal	Bioorg Med Chem Lett
Volume	21
Issue	23
Pages	7197-200
Date Published	2011 Dec 01
ISSN	1464-3405
DOI	10.1016/j.bmcl.2011.09.057
PubMed ID	22018462
Links
Grant list	1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States Howard Hughes Medical Institute / United States